Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine, Oct 26, 2016
Malaria infection is a major health burdens in Tropical Africa and this is made worst with the em... more Malaria infection is a major health burdens in Tropical Africa and this is made worst with the emergence of Plasmodium falciparum resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and 39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitrotribenzylamine derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase assay (pLDH). The result showed significant activity with IC50 ranging from 18 to 30 nM. The meta derivative (IC50:18.823 nM) showed better antiplasmodial activity than ortho (IC50: 30.287 nM) and para (IC50: 22.297 nM) derivatives, and even chloroquine phosphate (IC50: 22.777 nM).
Dihydroquinazolinones as Potential Antiproliferative and Tumor Inhibiting agents, Jul 27, 2016
2,3dihydroquinazolinone derivatives were screened for their antiproliferative activity, among all... more 2,3dihydroquinazolinone derivatives were screened for their antiproliferative activity, among all the synthesized molecules compound 3j with electron withdrawing substituents on phenyl ring displayed considerable cytotoxicity against HeLa, MCF7 and K562 cell lines with an IC50 value of 17.1, 31.5 and 25.3 µM, respectively. Further we carried out live dead fluorescence dye assay using calcein-AM and ethidium homodimer staining results further validate the capacity of compound 3j it induces apoptosis in HeLa cells. In addition, the potent compound 3j tested for tumor regression studies in Swiss albino mouse. Both in vitro and in vivo results revealed the significant antiproliferative activity of compound 3j in tumor cell lines and tumor tissue showed multifocal areas of necrosis and numerous number of apoptotic cells
Granular Cell Odontogenic Tumour - A Histopathological Rarity, Jun 28, 2016
Central Granular Cell Odontogenic Tumour (CGCOT) is an uncommon benign odontogenic neoplasm. It p... more Central Granular Cell Odontogenic Tumour (CGCOT) is an uncommon benign odontogenic neoplasm. It predominantly occurs in middle aged women. We report a case of CGCOT that occurred in the mandible of a 38 year old male patient. Clinical, radio graphical, histopathological features and immunohistochemical investigations like Calretinin, AE1/AE3, S100 and Neuron Specific Enolase (NSE) were described.
SVM based Prediction of Major Histocompatibility Complex Binders: Identification and Analysis of Dracunculus medinensis Peptide, Jun 22, 2016
The largest human infecting parasite causes guinea worm disease, known as the disease and cause o... more The largest human infecting parasite causes guinea worm disease, known as the disease and cause of poverty due to unavailability of the sanitized water. This is not lethal but causes the long term morbidity and motility in the infected human. In this research work, we predict the peptide binders of antigenic protein from D. medinensis sequence to MHC-I molecules are as 11mer_H2_Db, 10mer_H2_Db, 9mer_H2_Db, 8mer_H2_Db.Also study integrates prediction of peptide MHC class I binding; proteasomal C terminal cleavage and TAP transport efficiency by using sequence and properties of the amino acids. We also found the binding of peptides to different alleles by using Position Specific Scoring Matrix. NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis is 145 residues long with 137 nonamers having antigenic MHC binding peptides. PSSM based server will predict the peptide binders from D.medinensis of NADH dehydrogenase subunit 6 sequence to MHC-II molecules are as I_Ab.p, I_Ad.p, I_Ag7.p,I_Ak.p which are found antigenic epitopes region in NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis.
In Vitro Topoisomerase II Inhibitory and Apoptotic Activities of Novel 3,5 Disubstituted Thiophene-2- carboxylates, May 5, 2016
Topoisomerases (topoII) are crucial enzymes involved during DNA replication, repair and transcrip... more Topoisomerases (topoII) are crucial enzymes involved during DNA replication, repair and transcription. Recent studies have shown topo II as an interesting target for cancer therapy. In the current study we have synthesized and characterized few thiophene derivatives and determined their antiproliferative activity and apoptosis studies in cancer cell lines. Biochemical analysis showed that thiophene derivatives inhibit the alpha isoforms of topoisomerase II and hence these molecules can be considered as a potential anticancer drug.
New Routes for the Synthesis Novel Heterocyclic via Formation of C-N Bond and via Cleavage a Thiazine Ring of 1,4-Benzothiazine, Feb 4, 2016
The reactions of 2-aminothiophenol with acetylacetone in refluxing DMSO or ethanol was investigat... more The reactions of 2-aminothiophenol with acetylacetone in refluxing DMSO or ethanol was investigated. Treatment of 1 with enaminone 5 gave benzothiazine derivative 6. A reasonable mechanism to account for the formation of pyridone derivative 11 by treatment of 2 with malononitrile. Reactions of 2 with cyanoacetic hydrazide, thiosemicarbazide, and hydrazine hydrate and phenyl hydrazine afforded the compounds 13, 15 and, 17a-b respectively. Condensation of 13 with 4-methoxy benzaldehyde gave 18. The latter compound reacted with malononitrile gave pyridone derivative 19. A reasonable mechanism account for the formation of pyrazolo[3,4-b]pyridine derivative 20 from the reaction of 13 with DMF-DMA via cleavage of a thiazine ring of benzothiazine. The structures of all newly synthesized compounds elucidated by elemental analysis 1 H-NMR and 13 C-NMR spectra, Ms and X-ray crystallographic investigations. The reported crystal structures of these novel benzothiazine derivatives are expected to be a remarkable contribution to the crystallographic database of heterocyclic compounds.
Application of Heteropolyacids and Nano-Catalyst in Heterocycles Synthesis, Jan 28, 2016
Heteropolyacids (HPAs) possess unique properties such as: well-defined structure, Bronsted acidit... more Heteropolyacids (HPAs) possess unique properties such as: well-defined structure, Bronsted acidity, possibility to modify their acidbase and redox properties by changing their chemical composition (substituted HPAs), ability to accept and release electrons, high proton mobility, etc. In view of green chemistry, the substitution of harmful liquid acids by solid reusable HPAs as catalyst in organic synthesis is the most promising application of this acids. Heteropolyacids (HPAs) and related compounds have received considerable attention as solid acids in recent years. The application of heteropolyacids as catalytic materials is growing continuously in the catalytic field
Chemical and Biological Potentials of Chalcones: A Review, Dec 31, 2015
Plants from the natural world are linked with the treatment of different human ailments. This is ... more Plants from the natural world are linked with the treatment of different human ailments. This is due to the presence of different classes of chemical constituents. Flavonoids are one such class of natural constituents responsible for the activity of plants. Chalcones are a class of natural open chain flavonoids that are linked by a three carbon spacer between two aromatic rings. Chalcones and their heterocyclic analogues enjoy a range of biological activities such as antimicrobial, antioxidant, cytotoxic, anticancer, antiprotozoal, antihistaminic, antiulcer and antiinflammatory activities which makes these compounds as a special attraction for investigation. Additionally the bielectrophilic, ketovinyl chain between the two rings is highly reactive and acts as an important chemical synthon for constructing different five, six and seven membered heterocyclic scaffolds containing different hetero atoms like nitrogen, oxygen and sulfur atoms by abridgment with a variety of binucleophilic reagents. This review highlights on the chemical and biological potentials of chalcones
An Expedient One-Pot Synthetic Protocol to the Preparation Of Isoxazolo and Pyrazolo Annulated Analogues of Benzoxazepino Condensed Carbazoles and Azacarbazoles of Medicinal Interest, Nov 24, 2015
A facile one-pot synthetic protocol for the preparation of isoxazolo and pyrazolo annulated analo... more A facile one-pot synthetic protocol for the preparation of isoxazolo and pyrazolo annulated analogues of the benzoxazepine condensed carbazoles and azacarbazoles from the corresponding enolic ethers, α, β-unsaturated ketones, oxoketene dithioacetals and dimethylaminomethylene ketones derived from benzoxazepino condensed oxocarbazoles and oxoazacarbazoles has been described. Compounds were realized from the Japp-Klingemann reaction of the diazonium salt of 2-aminodibenzo [b,f] [1,4]oxazepine with 2-hydroxymethylideno cyclohexanone and N-benzyl-3-hydroxymethylidenopiperidin-4-one followed by Fischer indolization of the obtained hydrazone with kent’s acid. The synthesized heterocyclic compounds were characterized by IR, NMR and MS spectral data and in vitro antimicrobial activity of the synthesized compounds was screened against the standard bacterial and fungal strains. Some of these benzoxazepine derivatives have been found to display excellent antimicrobial activity against bacteria and fungi.
Is US Patent Policy Strong Enough to Withstand the Winds of Change: A Study of the Need to Change United States Patent Policy, Dec 3, 2015
The purpose of this case study was to learn how US patent policy requirements differ for the Soft... more The purpose of this case study was to learn how US patent policy requirements differ for the Software and Pharmaceutical Industries, specifically if United States Patent Policy adequately protects intellectual property rights [1] for two divergent industries while still encouraging research and development (R & D) investment sufficient to increase profits and innovation. Data for this study consisted of 38 witness testimonies delivered to US Congress between the years 2005 and 2010 by experts representing the two industries of interest: pharmaceutical and software. Key findings from the data analysis of these 38 testimonies revealed both within industry differences and between industry differences in patent law protection. Within industry differences showed variance based on size of the company and the degree to which they relied on their own R & D. Between industry differences reflected divergent ‘products’ with Pharmaceutical Industries needing long-term protection to recover R & D expenditures that include expenses for human trials research to proceed from patent application to market. Software industry, on the other hand, uses follow-on innovation of others to continue technological advancement by constantly improving upon existing software. The data show that these two industries use patent policy protection in different ways for different reasons. This information will enable Policymakers to develop another form of product protection in lieu of the current patent law to better meet the needs of these two industries rather than try to modify the existing law.
Synthesis and Antimalarial Properties of Three Substituted Trinitro-Tribenzylamine, Oct 26, 2016
Malaria infection is a major health burdens in Tropical Africa and this is made worst with the em... more Malaria infection is a major health burdens in Tropical Africa and this is made worst with the emergence of Plasmodium falciparum resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and 39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitrotribenzylamine derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase assay (pLDH). The result showed significant activity with IC50 ranging from 18 to 30 nM. The meta derivative (IC50:18.823 nM) showed better antiplasmodial activity than ortho (IC50: 30.287 nM) and para (IC50: 22.297 nM) derivatives, and even chloroquine phosphate (IC50: 22.777 nM).
Dihydroquinazolinones as Potential Antiproliferative and Tumor Inhibiting agents, Jul 27, 2016
2,3dihydroquinazolinone derivatives were screened for their antiproliferative activity, among all... more 2,3dihydroquinazolinone derivatives were screened for their antiproliferative activity, among all the synthesized molecules compound 3j with electron withdrawing substituents on phenyl ring displayed considerable cytotoxicity against HeLa, MCF7 and K562 cell lines with an IC50 value of 17.1, 31.5 and 25.3 µM, respectively. Further we carried out live dead fluorescence dye assay using calcein-AM and ethidium homodimer staining results further validate the capacity of compound 3j it induces apoptosis in HeLa cells. In addition, the potent compound 3j tested for tumor regression studies in Swiss albino mouse. Both in vitro and in vivo results revealed the significant antiproliferative activity of compound 3j in tumor cell lines and tumor tissue showed multifocal areas of necrosis and numerous number of apoptotic cells
Granular Cell Odontogenic Tumour - A Histopathological Rarity, Jun 28, 2016
Central Granular Cell Odontogenic Tumour (CGCOT) is an uncommon benign odontogenic neoplasm. It p... more Central Granular Cell Odontogenic Tumour (CGCOT) is an uncommon benign odontogenic neoplasm. It predominantly occurs in middle aged women. We report a case of CGCOT that occurred in the mandible of a 38 year old male patient. Clinical, radio graphical, histopathological features and immunohistochemical investigations like Calretinin, AE1/AE3, S100 and Neuron Specific Enolase (NSE) were described.
SVM based Prediction of Major Histocompatibility Complex Binders: Identification and Analysis of Dracunculus medinensis Peptide, Jun 22, 2016
The largest human infecting parasite causes guinea worm disease, known as the disease and cause o... more The largest human infecting parasite causes guinea worm disease, known as the disease and cause of poverty due to unavailability of the sanitized water. This is not lethal but causes the long term morbidity and motility in the infected human. In this research work, we predict the peptide binders of antigenic protein from D. medinensis sequence to MHC-I molecules are as 11mer_H2_Db, 10mer_H2_Db, 9mer_H2_Db, 8mer_H2_Db.Also study integrates prediction of peptide MHC class I binding; proteasomal C terminal cleavage and TAP transport efficiency by using sequence and properties of the amino acids. We also found the binding of peptides to different alleles by using Position Specific Scoring Matrix. NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis is 145 residues long with 137 nonamers having antigenic MHC binding peptides. PSSM based server will predict the peptide binders from D.medinensis of NADH dehydrogenase subunit 6 sequence to MHC-II molecules are as I_Ab.p, I_Ad.p, I_Ag7.p,I_Ak.p which are found antigenic epitopes region in NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis.
In Vitro Topoisomerase II Inhibitory and Apoptotic Activities of Novel 3,5 Disubstituted Thiophene-2- carboxylates, May 5, 2016
Topoisomerases (topoII) are crucial enzymes involved during DNA replication, repair and transcrip... more Topoisomerases (topoII) are crucial enzymes involved during DNA replication, repair and transcription. Recent studies have shown topo II as an interesting target for cancer therapy. In the current study we have synthesized and characterized few thiophene derivatives and determined their antiproliferative activity and apoptosis studies in cancer cell lines. Biochemical analysis showed that thiophene derivatives inhibit the alpha isoforms of topoisomerase II and hence these molecules can be considered as a potential anticancer drug.
New Routes for the Synthesis Novel Heterocyclic via Formation of C-N Bond and via Cleavage a Thiazine Ring of 1,4-Benzothiazine, Feb 4, 2016
The reactions of 2-aminothiophenol with acetylacetone in refluxing DMSO or ethanol was investigat... more The reactions of 2-aminothiophenol with acetylacetone in refluxing DMSO or ethanol was investigated. Treatment of 1 with enaminone 5 gave benzothiazine derivative 6. A reasonable mechanism to account for the formation of pyridone derivative 11 by treatment of 2 with malononitrile. Reactions of 2 with cyanoacetic hydrazide, thiosemicarbazide, and hydrazine hydrate and phenyl hydrazine afforded the compounds 13, 15 and, 17a-b respectively. Condensation of 13 with 4-methoxy benzaldehyde gave 18. The latter compound reacted with malononitrile gave pyridone derivative 19. A reasonable mechanism account for the formation of pyrazolo[3,4-b]pyridine derivative 20 from the reaction of 13 with DMF-DMA via cleavage of a thiazine ring of benzothiazine. The structures of all newly synthesized compounds elucidated by elemental analysis 1 H-NMR and 13 C-NMR spectra, Ms and X-ray crystallographic investigations. The reported crystal structures of these novel benzothiazine derivatives are expected to be a remarkable contribution to the crystallographic database of heterocyclic compounds.
Application of Heteropolyacids and Nano-Catalyst in Heterocycles Synthesis, Jan 28, 2016
Heteropolyacids (HPAs) possess unique properties such as: well-defined structure, Bronsted acidit... more Heteropolyacids (HPAs) possess unique properties such as: well-defined structure, Bronsted acidity, possibility to modify their acidbase and redox properties by changing their chemical composition (substituted HPAs), ability to accept and release electrons, high proton mobility, etc. In view of green chemistry, the substitution of harmful liquid acids by solid reusable HPAs as catalyst in organic synthesis is the most promising application of this acids. Heteropolyacids (HPAs) and related compounds have received considerable attention as solid acids in recent years. The application of heteropolyacids as catalytic materials is growing continuously in the catalytic field
Chemical and Biological Potentials of Chalcones: A Review, Dec 31, 2015
Plants from the natural world are linked with the treatment of different human ailments. This is ... more Plants from the natural world are linked with the treatment of different human ailments. This is due to the presence of different classes of chemical constituents. Flavonoids are one such class of natural constituents responsible for the activity of plants. Chalcones are a class of natural open chain flavonoids that are linked by a three carbon spacer between two aromatic rings. Chalcones and their heterocyclic analogues enjoy a range of biological activities such as antimicrobial, antioxidant, cytotoxic, anticancer, antiprotozoal, antihistaminic, antiulcer and antiinflammatory activities which makes these compounds as a special attraction for investigation. Additionally the bielectrophilic, ketovinyl chain between the two rings is highly reactive and acts as an important chemical synthon for constructing different five, six and seven membered heterocyclic scaffolds containing different hetero atoms like nitrogen, oxygen and sulfur atoms by abridgment with a variety of binucleophilic reagents. This review highlights on the chemical and biological potentials of chalcones
An Expedient One-Pot Synthetic Protocol to the Preparation Of Isoxazolo and Pyrazolo Annulated Analogues of Benzoxazepino Condensed Carbazoles and Azacarbazoles of Medicinal Interest, Nov 24, 2015
A facile one-pot synthetic protocol for the preparation of isoxazolo and pyrazolo annulated analo... more A facile one-pot synthetic protocol for the preparation of isoxazolo and pyrazolo annulated analogues of the benzoxazepine condensed carbazoles and azacarbazoles from the corresponding enolic ethers, α, β-unsaturated ketones, oxoketene dithioacetals and dimethylaminomethylene ketones derived from benzoxazepino condensed oxocarbazoles and oxoazacarbazoles has been described. Compounds were realized from the Japp-Klingemann reaction of the diazonium salt of 2-aminodibenzo [b,f] [1,4]oxazepine with 2-hydroxymethylideno cyclohexanone and N-benzyl-3-hydroxymethylidenopiperidin-4-one followed by Fischer indolization of the obtained hydrazone with kent’s acid. The synthesized heterocyclic compounds were characterized by IR, NMR and MS spectral data and in vitro antimicrobial activity of the synthesized compounds was screened against the standard bacterial and fungal strains. Some of these benzoxazepine derivatives have been found to display excellent antimicrobial activity against bacteria and fungi.
Is US Patent Policy Strong Enough to Withstand the Winds of Change: A Study of the Need to Change United States Patent Policy, Dec 3, 2015
The purpose of this case study was to learn how US patent policy requirements differ for the Soft... more The purpose of this case study was to learn how US patent policy requirements differ for the Software and Pharmaceutical Industries, specifically if United States Patent Policy adequately protects intellectual property rights [1] for two divergent industries while still encouraging research and development (R & D) investment sufficient to increase profits and innovation. Data for this study consisted of 38 witness testimonies delivered to US Congress between the years 2005 and 2010 by experts representing the two industries of interest: pharmaceutical and software. Key findings from the data analysis of these 38 testimonies revealed both within industry differences and between industry differences in patent law protection. Within industry differences showed variance based on size of the company and the degree to which they relied on their own R & D. Between industry differences reflected divergent ‘products’ with Pharmaceutical Industries needing long-term protection to recover R & D expenditures that include expenses for human trials research to proceed from patent application to market. Software industry, on the other hand, uses follow-on innovation of others to continue technological advancement by constantly improving upon existing software. The data show that these two industries use patent policy protection in different ways for different reasons. This information will enable Policymakers to develop another form of product protection in lieu of the current patent law to better meet the needs of these two industries rather than try to modify the existing law.
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resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro
tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and
39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitrotribenzylamine
derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase
assay (pLDH). The result showed significant activity with IC50 ranging from 18 to 30 nM. The meta derivative (IC50:18.823 nM) showed better
antiplasmodial activity than ortho (IC50: 30.287 nM) and para (IC50: 22.297 nM) derivatives, and even chloroquine phosphate (IC50: 22.777 nM).
with electron withdrawing substituents on phenyl ring displayed considerable cytotoxicity against HeLa, MCF7 and K562 cell lines with an IC50
value of 17.1, 31.5 and 25.3 µM, respectively. Further we carried out live dead fluorescence dye assay using calcein-AM and ethidium homodimer
staining results further validate the capacity of compound 3j it induces apoptosis in HeLa cells. In addition, the potent compound 3j tested for
tumor regression studies in Swiss albino mouse. Both in vitro and in vivo results revealed the significant antiproliferative activity of compound 3j
in tumor cell lines and tumor tissue showed multifocal areas of necrosis and numerous number of apoptotic cells
sanitized water. This is not lethal but causes the long term morbidity and motility in the infected human. In this research work, we predict
the peptide binders of antigenic protein from D. medinensis sequence to MHC-I molecules are as 11mer_H2_Db, 10mer_H2_Db, 9mer_H2_Db,
8mer_H2_Db.Also study integrates prediction of peptide MHC class I binding; proteasomal C terminal cleavage and TAP transport efficiency by using sequence and properties of the amino acids. We also found the binding of peptides to different alleles by using Position Specific Scoring
Matrix. NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis is 145 residues long with 137 nonamers having antigenic MHC binding peptides. PSSM based server will predict the peptide binders from D.medinensis of NADH dehydrogenase subunit 6 sequence to MHC-II molecules are as I_Ab.p, I_Ad.p, I_Ag7.p,I_Ak.p which are found antigenic epitopes region in NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis.
and redox properties by changing their chemical composition (substituted HPAs), ability to accept and release electrons, high proton
mobility, etc. In view of green chemistry, the substitution of harmful liquid acids by solid reusable HPAs as catalyst in organic synthesis is the
most promising application of this acids. Heteropolyacids (HPAs) and related compounds have received considerable attention as solid acids
in recent years. The application of heteropolyacids as catalytic materials is growing continuously in the catalytic field
of chemical constituents. Flavonoids are one such class of natural constituents responsible for the activity of plants. Chalcones are a class of
natural open chain flavonoids that are linked by a three carbon spacer between two aromatic rings. Chalcones and their heterocyclic analogues
enjoy a range of biological activities such as antimicrobial, antioxidant, cytotoxic, anticancer, antiprotozoal, antihistaminic, antiulcer and antiinflammatory
activities which makes these compounds as a special attraction for investigation. Additionally the bielectrophilic, ketovinyl
chain between the two rings is highly reactive and acts as an important chemical synthon for constructing different five, six and seven
membered heterocyclic scaffolds containing different hetero atoms like nitrogen, oxygen and sulfur atoms by abridgment with a variety of
binucleophilic reagents. This review highlights on the chemical and biological potentials of chalcones
specifically if United States Patent Policy adequately protects intellectual property rights [1] for two divergent industries while still
encouraging research and development (R & D) investment sufficient to increase profits and innovation. Data for this study consisted of
38 witness testimonies delivered to US Congress between the years 2005 and 2010 by experts representing the two industries of interest:
pharmaceutical and software. Key findings from the data analysis of these 38 testimonies revealed both within industry differences and
between industry differences in patent law protection. Within industry differences showed variance based on size of the company and the
degree to which they relied on their own R & D. Between industry differences reflected divergent ‘products’ with Pharmaceutical Industries
needing long-term protection to recover R & D expenditures that include expenses for human trials research to proceed from patent
application to market. Software industry, on the other hand, uses follow-on innovation of others to continue technological advancement
by constantly improving upon existing software. The data show that these two industries use patent policy protection in different ways for
different reasons. This information will enable Policymakers to develop another form of product protection in lieu of the current patent law
to better meet the needs of these two industries rather than try to modify the existing law.
resistance to the commonly used antimalarial drugs. There is therefore the need for new potent antimalarial drugs. Syntheses of o-trinitro
tribenzylamine (2TBN), m-trinitro tribenzylamine (3TBN) and p-trinitro tribenzylamine (4TBN) were carried and yields of 38.49%, 41.01% and
39.67% respectively were obtained on reacting the respective o-, m-, and p-nitro benzaldehyde with formamide. The three synthesized trinitrotribenzylamine
derivatives were tested in vitro against Plasmodium falciparum isolates (3D7 strain) using parasite lactate dehydrogenase
assay (pLDH). The result showed significant activity with IC50 ranging from 18 to 30 nM. The meta derivative (IC50:18.823 nM) showed better
antiplasmodial activity than ortho (IC50: 30.287 nM) and para (IC50: 22.297 nM) derivatives, and even chloroquine phosphate (IC50: 22.777 nM).
with electron withdrawing substituents on phenyl ring displayed considerable cytotoxicity against HeLa, MCF7 and K562 cell lines with an IC50
value of 17.1, 31.5 and 25.3 µM, respectively. Further we carried out live dead fluorescence dye assay using calcein-AM and ethidium homodimer
staining results further validate the capacity of compound 3j it induces apoptosis in HeLa cells. In addition, the potent compound 3j tested for
tumor regression studies in Swiss albino mouse. Both in vitro and in vivo results revealed the significant antiproliferative activity of compound 3j
in tumor cell lines and tumor tissue showed multifocal areas of necrosis and numerous number of apoptotic cells
sanitized water. This is not lethal but causes the long term morbidity and motility in the infected human. In this research work, we predict
the peptide binders of antigenic protein from D. medinensis sequence to MHC-I molecules are as 11mer_H2_Db, 10mer_H2_Db, 9mer_H2_Db,
8mer_H2_Db.Also study integrates prediction of peptide MHC class I binding; proteasomal C terminal cleavage and TAP transport efficiency by using sequence and properties of the amino acids. We also found the binding of peptides to different alleles by using Position Specific Scoring
Matrix. NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis is 145 residues long with 137 nonamers having antigenic MHC binding peptides. PSSM based server will predict the peptide binders from D.medinensis of NADH dehydrogenase subunit 6 sequence to MHC-II molecules are as I_Ab.p, I_Ad.p, I_Ag7.p,I_Ak.p which are found antigenic epitopes region in NADH dehydrogenase subunit 6 (mitochondrion) from D. medinensis.
and redox properties by changing their chemical composition (substituted HPAs), ability to accept and release electrons, high proton
mobility, etc. In view of green chemistry, the substitution of harmful liquid acids by solid reusable HPAs as catalyst in organic synthesis is the
most promising application of this acids. Heteropolyacids (HPAs) and related compounds have received considerable attention as solid acids
in recent years. The application of heteropolyacids as catalytic materials is growing continuously in the catalytic field
of chemical constituents. Flavonoids are one such class of natural constituents responsible for the activity of plants. Chalcones are a class of
natural open chain flavonoids that are linked by a three carbon spacer between two aromatic rings. Chalcones and their heterocyclic analogues
enjoy a range of biological activities such as antimicrobial, antioxidant, cytotoxic, anticancer, antiprotozoal, antihistaminic, antiulcer and antiinflammatory
activities which makes these compounds as a special attraction for investigation. Additionally the bielectrophilic, ketovinyl
chain between the two rings is highly reactive and acts as an important chemical synthon for constructing different five, six and seven
membered heterocyclic scaffolds containing different hetero atoms like nitrogen, oxygen and sulfur atoms by abridgment with a variety of
binucleophilic reagents. This review highlights on the chemical and biological potentials of chalcones
specifically if United States Patent Policy adequately protects intellectual property rights [1] for two divergent industries while still
encouraging research and development (R & D) investment sufficient to increase profits and innovation. Data for this study consisted of
38 witness testimonies delivered to US Congress between the years 2005 and 2010 by experts representing the two industries of interest:
pharmaceutical and software. Key findings from the data analysis of these 38 testimonies revealed both within industry differences and
between industry differences in patent law protection. Within industry differences showed variance based on size of the company and the
degree to which they relied on their own R & D. Between industry differences reflected divergent ‘products’ with Pharmaceutical Industries
needing long-term protection to recover R & D expenditures that include expenses for human trials research to proceed from patent
application to market. Software industry, on the other hand, uses follow-on innovation of others to continue technological advancement
by constantly improving upon existing software. The data show that these two industries use patent policy protection in different ways for
different reasons. This information will enable Policymakers to develop another form of product protection in lieu of the current patent law
to better meet the needs of these two industries rather than try to modify the existing law.