Russian Journal of Bioorganic Chemistry, May 15, 2014
ABSTRACT A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2... more ABSTRACT A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives were synthesized as antimicrobial agents using 7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methyl-4H-pyrido[3′,2′:4,5]thieno[3,2-d]-[1,3]oxazin-4-one as a starting compound. Its condensation with substituted aniline derivatives or phenyl hydrazine gave the corresponding N-substituted derivatives. Treatment of the starting compound with hydrazine hydrate afforded the corresponding N-amino derivative, which was reacted with substituted phenylisocyanate and phenylisothiocyanate derivatives to give the corresponding semicarbazides and thiosemicarbazide derivatives. All the newly synthesized compounds were evaluated for their antimicrobial activities in comparison to streptomycin and fusidic acid as positive controls. The structure assignments of the new compounds are based on chemical and spectroscopic evidence.
Bioorganic & Medicinal Chemistry Letters, 2015
Cyclohexyl thiosemicarbazone derivatives (C1-14) were synthesized, characterized and evaluated ag... more Cyclohexyl thiosemicarbazone derivatives (C1-14) were synthesized, characterized and evaluated against HER-2 over expressed breast cancer cells. The synthesized compounds were screened in vitro against four breast cancer cell lines; SKBr-3, MCF-7, MDA-MB-468 and MDA-MB-231. All the compounds showed activity against HER-2 over expressed SKBr-3 cells with (IC50=25.6±0.07μM-61.6±0.4μM). The most active compounds inhibit ALDH(+) breast cancer stem cells more effectively than the cancer stem cells specific agent Salinomycin. Immunohistochemistry staining also confirmed that these compounds inhibit the expression of HER-2 on SKBr-3 cells. Compound C2 significantly inhibited the cell migration and cell adhesion of breast cancer cell lines. Compound C2 was found to most active compound of this series targeting HER-2 over expressed breast cancer cells.
A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were... more A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were synthesized and evaluated as antiviral activities using 1-acetylpyrene as a starting material. The structure assignment of the new compounds was based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data and pharmacological activities of the synthesized compounds were reported.
Acta Crystallographica Section E Structure Reports Online, 2012
The triazoloquinazole ring system in the title compound, C15H10N4O2 is approximately planar (r.m.... more The triazoloquinazole ring system in the title compound, C15H10N4O2 is approximately planar (r.m.s. deviation = 0.035 Å). The phenyl ring of the phenoxy substitutent is aligned at 59.3 (1)° with respect to this ring system. In the crystal, two molecules are linked about a center of inversion by a pair of N—H...O hydrogen bonds, generating a dimer.
A series of Schiff bases 14–25 were designed and synthesized for evaluation of their antibacteria... more A series of Schiff bases 14–25 were designed and synthesized for evaluation of their antibacterial properties against multi-drug resistant bacteria (MDRB). The antibacterial activities of Schiff bases 14–25 showed that most of the synthesized compounds displayed a significant antibacterial activity. Assessment of in silico ADMET properties (absorption, distribution, metabolism, excretion and toxicity) of Schiff bases illustrates that all derivatives showed agreement to the Lipinski’s rule of five. Further enzymatic assay aided by molecular docking study demonstrated that compound 18 is a potent inhibitor of staphylococcus aureus DNA gyrase and dihydrofolate reductase kinases. This study could be valuable in the discovery of new potent antimicrobial agents.
To identify 650 patients who underwent CT for renal colic, and review them for age and gender, in... more To identify 650 patients who underwent CT for renal colic, and review them for age and gender, in Saudi Arabia. Scans were performed on a 16 multislice scanner. A total of 650 patients, with the clinical suspicion of ureteric colic were reviewed; 220 females (33.8%) and 430 males (66.2%), with a female to male ratio of 1:2. Exams were carried out from January 2005 to November 2006, at King Khalid University Hospital, Riyadh, Kingdom of Saudi Arabia. Three hundred and ninety five patients out of 650 had stones; 2 of 395 (0.5%) had stones in the 5-15 years age group, 28 (7.1%) in the 16-25 years age group, 99 (25.1%) in the 26-35 years, 106 (26.8%) in the 36-45 age group, 84 (21.9%) in the 46-55 age group, 51 (12.9%) in the 56-65 age group, and 25 (6.3%) in the above 66 years age group. The most significant finding in our study is that as the patients age increases so does the percentage of stones up to the age of 56, with a peak at age group of 26-35 where stone percentage reaches 26...
Novel reliable and cost-effective potentiometric screen-printed sensors for free bilirubin (BR) d... more Novel reliable and cost-effective potentiometric screen-printed sensors for free bilirubin (BR) detection were presented. The sensors were fabricated using ordered mesoporous carbon (OMC) as an ion-to-electron transducer. The ion-association complex [Ni(bphen)3]2+[BR]2− was utilized as a sensory recognition material in the plasticized Polyvinyl Chloride (PVC) membrane. The membrane was drop-casted on the OMC layer, which is attached on a carbon conductor (2-mm diameter). In a 50 mM phosphate solution of pH 8.5, the electrodes offered a Nernstian slope of −26.8 ± 1.1 (r2 = 0.9997) mV/decade with a range of linearity 1.0 × 10−6–1 × 10−2 M towards free bilirubin with a detection limit 8.8 × 10−7 M (0.52 µg/mL). The presented sensors offered good features in terms of reliability, ease of design, high potential stability, high specificity and good accuracy and precision. Chronopotentiometric and electrochemical impedance spectrometric measurements were used for short-term potential stabi...
Within a series of dipeptide derivatives (5–11), compound 4 was refluxed with d-glucose, d-xylose... more Within a series of dipeptide derivatives (5–11), compound 4 was refluxed with d-glucose, d-xylose, acetylacetone, diethylmalonate, carbon disulfide, ethyl cyanoacetate, and ethyl acetoacetate which yielded 5–11, respectively. The candidates 5–11 were characterized and their biological activities were evaluated where they showed different anti-microbial inhibitory activities based on the type of pathogenic microorganisms. Moreover, to understand modes of binding, molecular docking was used of Nicotinoylglycine derivatives with the active site of the penicillin-binding protein 3 (PBP3) and sterol 14-alpha demethylase’s (CYP51), and the results, which were achieved via covalent and non-covalent docking, were harmonized with the biological activity results. Therefore, it was extrapolated that compounds 4, 7, 8, 9, and 10 had good potential to inhibit sterol 14-alpha demethylase and penicillin-binding protein 3; consequently, these compounds are possibly suitable for the development of a...
Possible improvement of the performance characteristics, reliability and selectivity of solid-con... more Possible improvement of the performance characteristics, reliability and selectivity of solid-contact nitrate ion-selective electrodes (ISE) (SC/NO3−-ISE) is attained by the application of a nitron-nitrate (Nit+/NO3−) ion association complex and inserting multi-walled carbon nanotubes (MWCNTs) as an ion-to-electron transducer between the ion sensing membrane (ISM) and the electronic conductor glassy carbon (GC) substrate. The potentiometric performance of the proposed electrode revealed a Nernstian slope −55.1 ± 2.1 (r² = 0.997) mV/decade in the range from 8.0 × 10−8–1 × 10−2 M with a detection limit of 2.8 × 10−8 (1.7 ng/mL). Selectivity, repeatability and reproducibility of the proposed sensors were considerably improved as compared to the coated disc electrode (GC/NO3−-ISE) without insertion of a MWCNT layer. Short-term potential stability and capacitance of the proposed sensors were tested using a current-reversal chronopotentiometric technique. The potential drift in presence o...
International Journal of Immunopathology and Pharmacology
Diabetes patients suffer from chronic disorders in the metabolism due to high blood sugar caused ... more Diabetes patients suffer from chronic disorders in the metabolism due to high blood sugar caused by anomalies in insulin excretion. Recently, vanadium compounds have been prepared and functionalized to decrease the level of hyperglycemia. Vitamin A boosts beta cell activity; therefore, the lack of this vitamin plays a role in the development of type 2 diabetes. The aim of this article focused on the synthesis of a new anti-diabetic drug formed from the complexation of a vanadium(IV) salt with vitamin A. Vitamin A acts as a unidentate chelate through the oxygen of its –OH group. The vanadium(IV) compound is surrounded by two vitamin A molecules. The [VO(vitamin A)2(H2O)2] compound was synthesized in a binary solvent system consisting of MeOH/H2O (1:1 ratio) in alkaline media at pH = 8. This compound was characterized using Fourier transform infrared spectra (FT-IR), electronic spectra (UV–vis), effective magnetic moment, electron spin resonance (ESR), scanning electron microscopy (SE...
Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-dihydropyrimidine-2... more Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-dihydropyrimidine-2(1H)-one/thione derivatives (DHP1-9) were designed, synthesized, characterized and evaluated for antitumor activity against cancer stem cells. The compounds were synthesized in one pot. Enaminones E1 and E2 were reacted with substituted benzaldehydes and urea/thiourea in the presence of glacial acetic acid. The synthesized compounds were characterized by spectral analysis. The compounds were screened in vitro against colon cancer cell line (LOVO) colon cancer stem cells. Most of the compounds were found to be active against side population cancer stem cells with an inhibition of >50% at a 10 μM concentration. Compounds DHP-1, DHP-7 and DHP-9 were found to be inactive. Compound DHP-5 exhibited an in vitro anti-proliferative effect and arrested cancer cells at the Gap 2 phase (G2) checkpoint and demonstrated an inhibitory effect on tumor growth for a LOVO xenograft in a nude mouse exper...
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, Jan 30, 2016
New binuclear chromium (III) niacinamide compound with chemical formula [Cr2(Nic)(Cl)6(H2O)4]·H2O... more New binuclear chromium (III) niacinamide compound with chemical formula [Cr2(Nic)(Cl)6(H2O)4]·H2O was obtained upon the reaction of chromium (III) chloride with niacinamide (Nic) in methanol solvent at 60°C. The proposed structure was discussed with the help of microanalytical analyses, conductivity, spectroscopic (FT-IR and UV-vis.), magnetic calculations, thermogravimetric analyses (TG/TGA), and morphological studies (X-ray of solid powder and scan electron microscopy. The infrared spectrum of free niacinamide in comparison with its chromium (III) compound indicated that the chelation mode occurs via both nitrogen atoms of pyridine ring and primary -NH2 group. The efficiency of chromium (III) niacinamide compound in decreasing of glucose level of blood and HbA1c in case of diabetic rats was checked. The ameliorating gluconeogenic enzymes, lipid profile and antioxidant defense capacities are considered as an indicator of the efficiency of new chromium (III) compound as antidiabetic...
N-aryl phthalimides (1-10P) derived from thalidomide by insertion of hydrophobic groups were eval... more N-aryl phthalimides (1-10P) derived from thalidomide by insertion of hydrophobic groups were evaluated for anti-inflammatory activity and one compound (4-(1,3-dioxo-1,3-dihydro-2H- isoindol-2-yl)-N'-[(4-ethoxyphenyl)methylidene]benzohydrazide (6P)) was identified as a promising anti-inflammatory agent. Further testing confirmed that compared with the control, 6P treatment resulted in a considerable decrease in CD4+, NF-κB p65+, TNF-α+, IL-6+, GITR+ and IL-17+ cell populations and an increase in the Foxp3+, CD4+Foxp3+ and IκBα+ populations in whole blood and pleural fluid of a mouse model of lung inflammation. Moreover, treatment with the 6P compound decreased proteins associated with inflammation including TNF-α, IL-6, IL- 17, GITR, NF-κB, COX-2, STAT-3, and iNOS while increasing anti-inflammatory mediators such as IL-10 and IL-4. Histopathological examination confirmed the potent anti-inflammatory effects of the 6P compound. Thus, the phthalimide derivative 6P acts as a potent ...
The reaction of 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thione 5a,b and 10a,b with forma... more The reaction of 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thione 5a,b and 10a,b with formaldehyde solution and various primary aromatic amines or 1-substituted piperazines yielded the corresponding N-Mannich bases 6a-o, 7a-g and 11a-i. The newly synthesized N-Mannich bases 6a-o, 7a-g and 11a-i were tested for in vitro inhibitory activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. The compounds 6j, 6l, 6m, 7a, 7b, 7c, 7d, 7f, 11a, 11b, 11c, 11d, 11e, 11f, 11h and 11i displayed moderate to good activity against the tested Gram-positive bacteria, while compounds 7c, 11c, 11d, 11f and 11h showed potent broad spectrum antibacterial activity. None of the newly synthesized compounds were proved to possess marked activity against C. albicans.
Russian Journal of Bioorganic Chemistry, May 15, 2014
ABSTRACT A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2... more ABSTRACT A series of new 3-substituted-7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one derivatives were synthesized as antimicrobial agents using 7-(2-chloro-6-ethoxypyridin-4-yl)-9-(2,4-dichlorophenyl)-2-methyl-4H-pyrido[3′,2′:4,5]thieno[3,2-d]-[1,3]oxazin-4-one as a starting compound. Its condensation with substituted aniline derivatives or phenyl hydrazine gave the corresponding N-substituted derivatives. Treatment of the starting compound with hydrazine hydrate afforded the corresponding N-amino derivative, which was reacted with substituted phenylisocyanate and phenylisothiocyanate derivatives to give the corresponding semicarbazides and thiosemicarbazide derivatives. All the newly synthesized compounds were evaluated for their antimicrobial activities in comparison to streptomycin and fusidic acid as positive controls. The structure assignments of the new compounds are based on chemical and spectroscopic evidence.
Bioorganic & Medicinal Chemistry Letters, 2015
Cyclohexyl thiosemicarbazone derivatives (C1-14) were synthesized, characterized and evaluated ag... more Cyclohexyl thiosemicarbazone derivatives (C1-14) were synthesized, characterized and evaluated against HER-2 over expressed breast cancer cells. The synthesized compounds were screened in vitro against four breast cancer cell lines; SKBr-3, MCF-7, MDA-MB-468 and MDA-MB-231. All the compounds showed activity against HER-2 over expressed SKBr-3 cells with (IC50=25.6±0.07μM-61.6±0.4μM). The most active compounds inhibit ALDH(+) breast cancer stem cells more effectively than the cancer stem cells specific agent Salinomycin. Immunohistochemistry staining also confirmed that these compounds inhibit the expression of HER-2 on SKBr-3 cells. Compound C2 significantly inhibited the cell migration and cell adhesion of breast cancer cell lines. Compound C2 was found to most active compound of this series targeting HER-2 over expressed breast cancer cells.
A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were... more A series of substituted pyrene derivatives 2–15 incorporated heterocyclic and sugar moieties were synthesized and evaluated as antiviral activities using 1-acetylpyrene as a starting material. The structure assignment of the new compounds was based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data and pharmacological activities of the synthesized compounds were reported.
Acta Crystallographica Section E Structure Reports Online, 2012
The triazoloquinazole ring system in the title compound, C15H10N4O2 is approximately planar (r.m.... more The triazoloquinazole ring system in the title compound, C15H10N4O2 is approximately planar (r.m.s. deviation = 0.035 Å). The phenyl ring of the phenoxy substitutent is aligned at 59.3 (1)° with respect to this ring system. In the crystal, two molecules are linked about a center of inversion by a pair of N—H...O hydrogen bonds, generating a dimer.
A series of Schiff bases 14–25 were designed and synthesized for evaluation of their antibacteria... more A series of Schiff bases 14–25 were designed and synthesized for evaluation of their antibacterial properties against multi-drug resistant bacteria (MDRB). The antibacterial activities of Schiff bases 14–25 showed that most of the synthesized compounds displayed a significant antibacterial activity. Assessment of in silico ADMET properties (absorption, distribution, metabolism, excretion and toxicity) of Schiff bases illustrates that all derivatives showed agreement to the Lipinski’s rule of five. Further enzymatic assay aided by molecular docking study demonstrated that compound 18 is a potent inhibitor of staphylococcus aureus DNA gyrase and dihydrofolate reductase kinases. This study could be valuable in the discovery of new potent antimicrobial agents.
To identify 650 patients who underwent CT for renal colic, and review them for age and gender, in... more To identify 650 patients who underwent CT for renal colic, and review them for age and gender, in Saudi Arabia. Scans were performed on a 16 multislice scanner. A total of 650 patients, with the clinical suspicion of ureteric colic were reviewed; 220 females (33.8%) and 430 males (66.2%), with a female to male ratio of 1:2. Exams were carried out from January 2005 to November 2006, at King Khalid University Hospital, Riyadh, Kingdom of Saudi Arabia. Three hundred and ninety five patients out of 650 had stones; 2 of 395 (0.5%) had stones in the 5-15 years age group, 28 (7.1%) in the 16-25 years age group, 99 (25.1%) in the 26-35 years, 106 (26.8%) in the 36-45 age group, 84 (21.9%) in the 46-55 age group, 51 (12.9%) in the 56-65 age group, and 25 (6.3%) in the above 66 years age group. The most significant finding in our study is that as the patients age increases so does the percentage of stones up to the age of 56, with a peak at age group of 26-35 where stone percentage reaches 26...
Novel reliable and cost-effective potentiometric screen-printed sensors for free bilirubin (BR) d... more Novel reliable and cost-effective potentiometric screen-printed sensors for free bilirubin (BR) detection were presented. The sensors were fabricated using ordered mesoporous carbon (OMC) as an ion-to-electron transducer. The ion-association complex [Ni(bphen)3]2+[BR]2− was utilized as a sensory recognition material in the plasticized Polyvinyl Chloride (PVC) membrane. The membrane was drop-casted on the OMC layer, which is attached on a carbon conductor (2-mm diameter). In a 50 mM phosphate solution of pH 8.5, the electrodes offered a Nernstian slope of −26.8 ± 1.1 (r2 = 0.9997) mV/decade with a range of linearity 1.0 × 10−6–1 × 10−2 M towards free bilirubin with a detection limit 8.8 × 10−7 M (0.52 µg/mL). The presented sensors offered good features in terms of reliability, ease of design, high potential stability, high specificity and good accuracy and precision. Chronopotentiometric and electrochemical impedance spectrometric measurements were used for short-term potential stabi...
Within a series of dipeptide derivatives (5–11), compound 4 was refluxed with d-glucose, d-xylose... more Within a series of dipeptide derivatives (5–11), compound 4 was refluxed with d-glucose, d-xylose, acetylacetone, diethylmalonate, carbon disulfide, ethyl cyanoacetate, and ethyl acetoacetate which yielded 5–11, respectively. The candidates 5–11 were characterized and their biological activities were evaluated where they showed different anti-microbial inhibitory activities based on the type of pathogenic microorganisms. Moreover, to understand modes of binding, molecular docking was used of Nicotinoylglycine derivatives with the active site of the penicillin-binding protein 3 (PBP3) and sterol 14-alpha demethylase’s (CYP51), and the results, which were achieved via covalent and non-covalent docking, were harmonized with the biological activity results. Therefore, it was extrapolated that compounds 4, 7, 8, 9, and 10 had good potential to inhibit sterol 14-alpha demethylase and penicillin-binding protein 3; consequently, these compounds are possibly suitable for the development of a...
Possible improvement of the performance characteristics, reliability and selectivity of solid-con... more Possible improvement of the performance characteristics, reliability and selectivity of solid-contact nitrate ion-selective electrodes (ISE) (SC/NO3−-ISE) is attained by the application of a nitron-nitrate (Nit+/NO3−) ion association complex and inserting multi-walled carbon nanotubes (MWCNTs) as an ion-to-electron transducer between the ion sensing membrane (ISM) and the electronic conductor glassy carbon (GC) substrate. The potentiometric performance of the proposed electrode revealed a Nernstian slope −55.1 ± 2.1 (r² = 0.997) mV/decade in the range from 8.0 × 10−8–1 × 10−2 M with a detection limit of 2.8 × 10−8 (1.7 ng/mL). Selectivity, repeatability and reproducibility of the proposed sensors were considerably improved as compared to the coated disc electrode (GC/NO3−-ISE) without insertion of a MWCNT layer. Short-term potential stability and capacitance of the proposed sensors were tested using a current-reversal chronopotentiometric technique. The potential drift in presence o...
International Journal of Immunopathology and Pharmacology
Diabetes patients suffer from chronic disorders in the metabolism due to high blood sugar caused ... more Diabetes patients suffer from chronic disorders in the metabolism due to high blood sugar caused by anomalies in insulin excretion. Recently, vanadium compounds have been prepared and functionalized to decrease the level of hyperglycemia. Vitamin A boosts beta cell activity; therefore, the lack of this vitamin plays a role in the development of type 2 diabetes. The aim of this article focused on the synthesis of a new anti-diabetic drug formed from the complexation of a vanadium(IV) salt with vitamin A. Vitamin A acts as a unidentate chelate through the oxygen of its –OH group. The vanadium(IV) compound is surrounded by two vitamin A molecules. The [VO(vitamin A)2(H2O)2] compound was synthesized in a binary solvent system consisting of MeOH/H2O (1:1 ratio) in alkaline media at pH = 8. This compound was characterized using Fourier transform infrared spectra (FT-IR), electronic spectra (UV–vis), effective magnetic moment, electron spin resonance (ESR), scanning electron microscopy (SE...
Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-dihydropyrimidine-2... more Novel 4-(4-substituted phenyl)-5-(3,4,5-trimethoxy/3,4-dimethoxy)-benzoyl-3,4-dihydropyrimidine-2(1H)-one/thione derivatives (DHP1-9) were designed, synthesized, characterized and evaluated for antitumor activity against cancer stem cells. The compounds were synthesized in one pot. Enaminones E1 and E2 were reacted with substituted benzaldehydes and urea/thiourea in the presence of glacial acetic acid. The synthesized compounds were characterized by spectral analysis. The compounds were screened in vitro against colon cancer cell line (LOVO) colon cancer stem cells. Most of the compounds were found to be active against side population cancer stem cells with an inhibition of >50% at a 10 μM concentration. Compounds DHP-1, DHP-7 and DHP-9 were found to be inactive. Compound DHP-5 exhibited an in vitro anti-proliferative effect and arrested cancer cells at the Gap 2 phase (G2) checkpoint and demonstrated an inhibitory effect on tumor growth for a LOVO xenograft in a nude mouse exper...
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, Jan 30, 2016
New binuclear chromium (III) niacinamide compound with chemical formula [Cr2(Nic)(Cl)6(H2O)4]·H2O... more New binuclear chromium (III) niacinamide compound with chemical formula [Cr2(Nic)(Cl)6(H2O)4]·H2O was obtained upon the reaction of chromium (III) chloride with niacinamide (Nic) in methanol solvent at 60°C. The proposed structure was discussed with the help of microanalytical analyses, conductivity, spectroscopic (FT-IR and UV-vis.), magnetic calculations, thermogravimetric analyses (TG/TGA), and morphological studies (X-ray of solid powder and scan electron microscopy. The infrared spectrum of free niacinamide in comparison with its chromium (III) compound indicated that the chelation mode occurs via both nitrogen atoms of pyridine ring and primary -NH2 group. The efficiency of chromium (III) niacinamide compound in decreasing of glucose level of blood and HbA1c in case of diabetic rats was checked. The ameliorating gluconeogenic enzymes, lipid profile and antioxidant defense capacities are considered as an indicator of the efficiency of new chromium (III) compound as antidiabetic...
N-aryl phthalimides (1-10P) derived from thalidomide by insertion of hydrophobic groups were eval... more N-aryl phthalimides (1-10P) derived from thalidomide by insertion of hydrophobic groups were evaluated for anti-inflammatory activity and one compound (4-(1,3-dioxo-1,3-dihydro-2H- isoindol-2-yl)-N'-[(4-ethoxyphenyl)methylidene]benzohydrazide (6P)) was identified as a promising anti-inflammatory agent. Further testing confirmed that compared with the control, 6P treatment resulted in a considerable decrease in CD4+, NF-κB p65+, TNF-α+, IL-6+, GITR+ and IL-17+ cell populations and an increase in the Foxp3+, CD4+Foxp3+ and IκBα+ populations in whole blood and pleural fluid of a mouse model of lung inflammation. Moreover, treatment with the 6P compound decreased proteins associated with inflammation including TNF-α, IL-6, IL- 17, GITR, NF-κB, COX-2, STAT-3, and iNOS while increasing anti-inflammatory mediators such as IL-10 and IL-4. Histopathological examination confirmed the potent anti-inflammatory effects of the 6P compound. Thus, the phthalimide derivative 6P acts as a potent ...
The reaction of 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thione 5a,b and 10a,b with forma... more The reaction of 5-(1-adamantyl)-4-substituted-1,2,4-triazoline-3-thione 5a,b and 10a,b with formaldehyde solution and various primary aromatic amines or 1-substituted piperazines yielded the corresponding N-Mannich bases 6a-o, 7a-g and 11a-i. The newly synthesized N-Mannich bases 6a-o, 7a-g and 11a-i were tested for in vitro inhibitory activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. The compounds 6j, 6l, 6m, 7a, 7b, 7c, 7d, 7f, 11a, 11b, 11c, 11d, 11e, 11f, 11h and 11i displayed moderate to good activity against the tested Gram-positive bacteria, while compounds 7c, 11c, 11d, 11f and 11h showed potent broad spectrum antibacterial activity. None of the newly synthesized compounds were proved to possess marked activity against C. albicans.
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