Molecules

91 KiB

Open AccessArticle

First Synthesis and Isolation of the E- and Z-Isomers of Some New Schiff Bases. Reactions of 6-Azido-5-Formyl-2-Pyridone with Aromatic Amines

by Ramadan A. Mekheimer, Afaf M. Abdel Hameed and Kamal U. Sadek

Molecules 2008, 13(1), 195-203; https://doi.org/10.3390/molecules13010195 - 30 Jan 2008

Cited by 2 | Viewed by 8838

Abstract

Some novel Schiff bases have been prepared by reacting 6-azido-5-formyl-2-pyridone 1 with a series of aromatic amines 2a-f. 5-Arylaminomethylene-6-(E)-aryliminopyridones3a-e were obtained by reaction of 1 with 2a-e at room temperature,whereas with 2f, the 6-azido-5-naphthalen-2-yl-iminomethylpyridone derivative 4 wasformed. On the other hand, heating 1 [...] Read more.

Some novel Schiff bases have been prepared by reacting 6-azido-5-formyl-2-pyridone 1 with a series of aromatic amines 2a-f. 5-Arylaminomethylene-6-(E)-aryliminopyridones3a-e were obtained by reaction of 1 with 2a-e at room temperature,whereas with 2f, the 6-azido-5-naphthalen-2-yl-iminomethylpyridone derivative 4 wasformed. On the other hand, heating 1 with 2a-d at 140-150°C yielded two sets of isomericproducts, (E)-3a-d and (Z)-5a-d. Refluxing compounds (Z)-3a,c with hydroxyl-amine inmethanol gave the corresponding hydroxyliminopyridones 8a,c. Heating of (E)-3a-d withexcess POCl3 at reflux did not give the expected tricyclic compound 9, but rather theisomeric products (Z)-5a-d were obtained. The structures of all these products have beencharacterized using IR and 1H- and 13C-NMR spectroscopy. Full article

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136 KiB

Open AccessArticle

Chemical Composition of Ground Pearl (Eurhizococcus colombianus) Cysts

by Winston Quiñones, Bernardo Vicente, Fernando Torres, Rosendo Archbold, Walter Murillo, Martha Londoño and Fernando Echeverri

Molecules 2008, 13(1), 190-194; https://doi.org/10.3390/molecules13010190 - 29 Jan 2008

Cited by 3 | Viewed by 10601

Abstract

Ground pearl (Eurhizococcus colombianus) is a crop pest in Colombia, withspecial impact on fig, grass, rubus and tomato plants. The insect is resistant to externalinsecticide application because it produces a thick waxy shell that isolates it from theenvironment. The composition of this shell [...] Read more.

Ground pearl (Eurhizococcus colombianus) is a crop pest in Colombia, withspecial impact on fig, grass, rubus and tomato plants. The insect is resistant to externalinsecticide application because it produces a thick waxy shell that isolates it from theenvironment. The composition of this shell was determined by NMR and MS as atriglyceride, whose fatty acid is transformed into other products with the metamorphosis ofthe insect. Additionally, several enzymatic inhibitors were assayed to control the insectwith negative results. Full article

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247 KiB

Open AccessArticle

New Di-(β-chloroethyl)-α-amides on N-(meta-Acylaminobenzoyl)- D,L-aminoacid Supports with Antitumoral Activity

by Valeriu Sunel, Marcel Popa, Jacques Desbrières, Lenuta Profire, Pintilie Otilia and Lionte Catalina

Molecules 2008, 13(1), 177-189; https://doi.org/10.3390/molecules13010177 - 28 Jan 2008

Cited by 12 | Viewed by 9866

Abstract

In order to obtain new compounds with antitumoural action the N-(metaacylaminobenzoyl)-α-acylaminobenzoyl)-α-aminoacids 4-9 were prepared. Thesecompounds were subsequently converted into the corresponding δ²-oxazolin-5-ones 10-15,which in turn were submitted to a ring opening reaction with di-(β-chloroethyl)amine toafford the peptide supported N-mustards 16-21, which [...] Read more.

In order to obtain new compounds with antitumoural action the N-(metaacylaminobenzoyl)-α-acylaminobenzoyl)-α-aminoacids 4-9 were prepared. Thesecompounds were subsequently converted into the corresponding δ²-oxazolin-5-ones 10-15,which in turn were submitted to a ring opening reaction with di-(β-chloroethyl)amine toafford the peptide supported N-mustards 16-21, which showed low toxicity and cytostaticactivity similar to that of sarcolisine against the Ehrlich ascite and Walker 253carcinosarcoma. Full article

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63 KiB

Open AccessArticle

Reaction of Nitrilimines with 2-Substituted Aza-heterocycles. Synthesis of Pyrrolo[1,2-a]pyridine and Pyrimido[2,1-d]1,2,3,5- tetrazine

by Adel M. Awadallah and Jalal A. Zahra

Molecules 2008, 13(1), 170-176; https://doi.org/10.3390/molecules13010170 - 28 Jan 2008

Cited by 9 | Viewed by 8922

Abstract

The reaction of nitrilimine 6a with ethyl pyridine-2-acetate (7) gave thecorresponding pyrrolo[1,2-a]pyridine 8, while the reaction of 6b containing an estermoiety afforded the acyclic adduct 9. The reaction of 6a with 2-aminopyrimidine (10)gave the novel unexpected pyrimido[2,1-d]1,2,3,5-tetrazine 11. Acyclic adducts 16 and17 were [...] Read more.

The reaction of nitrilimine 6a with ethyl pyridine-2-acetate (7) gave thecorresponding pyrrolo[1,2-a]pyridine 8, while the reaction of 6b containing an estermoiety afforded the acyclic adduct 9. The reaction of 6a with 2-aminopyrimidine (10)gave the novel unexpected pyrimido[2,1-d]1,2,3,5-tetrazine 11. Acyclic adducts 16 and17 were obtained from the reaction of 6b with 2-cyanomethylbenzimidazole (14) and 2-aminobenzimidazole (15), respectively. Full article

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Open AccessArticle

The Synthesis of Unsubstituted Cyclic Imides Using Hydroxylamine under Microwave Irradiation

by Ellis Benjamin and Yousef Hijji

Molecules 2008, 13(1), 157-169; https://doi.org/10.3390/molecules13010157 - 25 Jan 2008

Cited by 34 | Viewed by 12098

Abstract

Unsubstituted cyclic imides were synthesized from a series of cyclic anhydrides,hydroxylamine hydrochloride (NH2OH·HCl), and 4-N,N-dimethylamino-pyridine (DMAP,base catalyst) under microwave irradiation in monomode and multimode microwaves. Thisnovel microwave synthesis produced high yields of the unsubstituted cyclic imides forboth the monomode (61 - 81%) and [...] Read more.

Unsubstituted cyclic imides were synthesized from a series of cyclic anhydrides,hydroxylamine hydrochloride (NH2OH·HCl), and 4-N,N-dimethylamino-pyridine (DMAP,base catalyst) under microwave irradiation in monomode and multimode microwaves. Thisnovel microwave synthesis produced high yields of the unsubstituted cyclic imides forboth the monomode (61 - 81%) and multimode (84 - 97%) microwaves. Full article

(This article belongs to the Section Organic Chemistry)

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47 KiB

Open AccessArticle

Preparation of Second Generation Ionic Liquids by Efficient Solvent-Free Alkylation of N-Heterocycles with Chloroalkanes

by Giancarlo Cravotto, Emanuela Calcio Gaudino, Luisa Boffa, Jean-Marc Lévêque, Julien Estager and Werner Bonrath

Molecules 2008, 13(1), 149-156; https://doi.org/10.3390/molecules13010149 - 25 Jan 2008

Cited by 53 | Viewed by 15404

Abstract

Non-conventional techniques, such as microwave (MW) and power ultrasound(US) as well as combined MW/US irradiation, have been used to promote one-potsynthesis of second-generation ionic liquids (ILs), cutting down reaction times andimproving yields. However, the use of chloroalkanes in the alkylation of N-heterocyclesrequires more [...] Read more.

Non-conventional techniques, such as microwave (MW) and power ultrasound(US) as well as combined MW/US irradiation, have been used to promote one-potsynthesis of second-generation ionic liquids (ILs), cutting down reaction times andimproving yields. However, the use of chloroalkanes in the alkylation of N-heterocyclesrequires more drastic conditions if results are to match those obtained with more reactivealkyl halides. The present paper describes a series of MW- or MW/US-promoted ILpreparations starting from chloroalkanes and classic heterocycles (1-methylimidazole,pyridine and 1-methylpyrrolidine). When reactions were carried out under conventionalheating in an oil bath they required longer reaction times and gave poorer yields. ¹H-NMRanalysis and ion-exchange chromatography showed that the present solventless procedureafforded ILs of satisfactory purity. The observed high yields (usually 70-98% isolated),and short reaction times showed that a straightforward access to ILs can be also achievedwith the use of alkyl chlorides, resulting in a considerable reduction of costs. Full article

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Open AccessArticle

Asymmetric Biomimetic Oxidations of Phenols: The Mechanism of the Diastereo- and Enantioselective Synthesis of Thomasidioic Acid

by Luca Zoia, Maurizio Bruschi, Marco Orlandi, Eeva-Liisa Tolppa and Bruno Rindone

Molecules 2008, 13(1), 129-148; https://doi.org/10.3390/molecules13010129 - 23 Jan 2008

Cited by 14 | Viewed by 8551

Abstract

Enantiopure chiral amidic derivatives of sinapic acid were oxidised withhydrogen peroxide using horseradish peroxidase (HRP) as the catalyst to give thearyltetraline dilignol thomasidioic acid. Trans-diastereoselectivity and enantioselectivity inthe formation of thomasidioic acid was observed. Computational methods show that theenantioselectivity is controlled by the [...] Read more.

Enantiopure chiral amidic derivatives of sinapic acid were oxidised withhydrogen peroxide using horseradish peroxidase (HRP) as the catalyst to give thearyltetraline dilignol thomasidioic acid. Trans-diastereoselectivity and enantioselectivity inthe formation of thomasidioic acid was observed. Computational methods show that theenantioselectivity is controlled by the β-β oxidative coupling step, while thediastereoselectivity is controlled by the stability of the reactive conformation of theintermediate quinomethide. Full article

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204 KiB

Open AccessArticle

Antiplatelet Aggregation Coumarins from the Leaves of Murraya omphalocarpa

by Yi-Chen Chia, Fang-Rong Chang, Jinn-Chyi Wang, Chin-Chung Wu, Michael Y.-N. Chiang, Yu-Hsuan Lan, Keh-Shaw Chen and Yang-Chang Wu

Molecules 2008, 13(1), 122-128; https://doi.org/10.3390/molecules13010122 - 21 Jan 2008

Cited by 25 | Viewed by 11022

Abstract

Using a bioactivity-guided fractionation method, two coumarins: minumicrolineacetonide (1) and epimurpaniculol senecioate (2), were isolated from the leaves ofMurraya omphalocarpa Hayata (Rutaceae). Compound 1 had been previously synthesizedand was now isolated from natural sources for the first time, and compound 2, possessing anegative [...] Read more.

Using a bioactivity-guided fractionation method, two coumarins: minumicrolineacetonide (1) and epimurpaniculol senecioate (2), were isolated from the leaves ofMurraya omphalocarpa Hayata (Rutaceae). Compound 1 had been previously synthesizedand was now isolated from natural sources for the first time, and compound 2, possessing anegative optical rotation value, is new. The structures and their stereochemistry were fullyelucidated on the basis of spectroscopic and X-ray crystallographic techniques. Bothcompounds 1 and 2 are active in the antiplatelet aggregation assay. Interestingly, thepossible acetonide artifact 1 displayed significant antiplatelet aggregation induced not onlyby AA and collagen but also by platelet activating factor (PAF). Full article

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Open AccessArticle

Synthesis, Acidity and Antioxidant Properties of Some Novel 3,4-disubstituted-4,5-dihydro-1H-1,2,4-triazol-5-one Derivatives

by Muzaffer Alkan, Haydar Yüksek, Özlem Gürsoy-Kol and Mustafa Calapoğlu

Molecules 2008, 13(1), 107-121; https://doi.org/10.3390/molecules13010107 - 19 Jan 2008

Cited by 33 | Viewed by 8670

Abstract

3-Alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones 2a-g reacted with4-diethylaminobenzaldehyde to afford the corresponding 3-alkyl(aryl)-4-(4-diethylaminobenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones 3a-g. The acetylationreactions of compounds 3a-e were investigated and compounds 4a-e were thus obtained.The new compounds were characterized using IR, ¹H-NMR, ¹³C-NMR, UV and MSspectral data. In addition, the newly synthesized compounds [...] Read more.

3-Alkyl(aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones 2a-g reacted with4-diethylaminobenzaldehyde to afford the corresponding 3-alkyl(aryl)-4-(4-diethylaminobenzylidenamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones 3a-g. The acetylationreactions of compounds 3a-e were investigated and compounds 4a-e were thus obtained.The new compounds were characterized using IR, ¹H-NMR, ¹³C-NMR, UV and MSspectral data. In addition, the newly synthesized compounds 3a-g were titratedpotentiometrically with tetrabutylammonium hydroxide in four non-aqueous solvents suchas isopropyl alcohol, tert-butyl alcohol, acetone and N,N-dimethylformamide (DMF), andthe half-neutralization potential values and the corresponding pKa values were determinedfor all cases. Moreover, 3 and 4 type compounds were also screened for their antioxidantactivities. Full article

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101 KiB

Open AccessArticle

Synthesis and Structural Analysis of Polyester Prodrugs of Norfloxacin

by Marcin Sobczak, Ewa Witkowska, Ewa Olędzka and Waclaw Kolodziejski

Molecules 2008, 13(1), 96-106; https://doi.org/10.3390/molecules13010096 - 18 Jan 2008

Cited by 45 | Viewed by 10024

Abstract

Two-, three- and four-arm, star-shaped poly(ε-caprolactone) andpoly(D,L-lactide) homopolymers, and copolymers of ε-caprolactone with D,L-lactide weresynthesized via ring-opening polymerization of cyclic esters in the presence of glycerol,penthaerythritol and poly(ethylene glycol) as initiators and stannous octoate as a catalyst.Thus obtained oligomers were successfully used in [...] Read more.

Two-, three- and four-arm, star-shaped poly(ε-caprolactone) andpoly(D,L-lactide) homopolymers, and copolymers of ε-caprolactone with D,L-lactide weresynthesized via ring-opening polymerization of cyclic esters in the presence of glycerol,penthaerythritol and poly(ethylene glycol) as initiators and stannous octoate as a catalyst.Thus obtained oligomers were successfully used in the synthesis of novel macromolecularprodrugs of norfloxacin. The structures of the polymers and prodrugs were elucidated bymeans of MALDI-TOF MS, NMR and IR studies. Full article

(This article belongs to the Section Medicinal Chemistry)

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72 KiB

Open AccessArticle

Substitutions of Fluorine Atoms and Phenoxy Groups in the Synthesis of Quinoxaline 1,4-di-N-oxide Derivatives

by Esther Vicente, Raquel Villar, Asunción Burguete, Beatriz Solano, Saioa Ancizu, Silvia Pérez-Silanes, Ignacio Aldana and Antonio Monge

Molecules 2008, 13(1), 86-95; https://doi.org/10.3390/molecules13010086 - 18 Jan 2008

Cited by 11 | Viewed by 10152

Abstract

The unexpected substitution of fluorine atoms and phenoxy groups attached toquinoxaline or benzofuroxan rings is described. The synthesis of 2-benzyl- and 2-phenoxy-3-methylquinoxaline 1,4-di-N-oxide derivatives was based on the classical Beirut reaction.The tendency of fluorine atoms linked to quinoxaline or benzofuroxan rings to be [...] Read more.

The unexpected substitution of fluorine atoms and phenoxy groups attached toquinoxaline or benzofuroxan rings is described. The synthesis of 2-benzyl- and 2-phenoxy-3-methylquinoxaline 1,4-di-N-oxide derivatives was based on the classical Beirut reaction.The tendency of fluorine atoms linked to quinoxaline or benzofuroxan rings to be replacedby a methoxy group when dissolved in an ammonia saturated solution of methanol wasclearly demonstrated. In addition, 2-phenoxyquinoxaline 1,4-di-N-oxide derivativesbecame 2-aminoquinoxaline 1,4-di-N-oxide derivatives in the presence of gaseousammonia. Full article

(This article belongs to the Section Organic Chemistry)

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Open AccessArticle

Unexpected Reduction of Ethyl 3-Phenylquinoxaline-2- carboxylate 1,4-Di-N-oxide Derivatives by Amines

by Lidia M. Lima, Esther Vicente, Beatriz Solano, Silvia Pérez-Silanes, Ignacio Aldana and Antonio Monge

Molecules 2008, 13(1), 78-85; https://doi.org/10.3390/molecules13010078 - 17 Jan 2008

Cited by 9 | Viewed by 12511

Abstract

The unexpected tendency of amines and functionalized hydrazines to reduceethyl 3-phenylquinoxaline-2-carboxylate 1,4-di-N-oxide (1) to afford a quinoxaline 1c andmono-oxide quinoxalines 1a and 1b is described. The experimental conditions werestandardized to the use of two equivalents of amine in ethanol under reflux for two [...] Read more.

The unexpected tendency of amines and functionalized hydrazines to reduceethyl 3-phenylquinoxaline-2-carboxylate 1,4-di-N-oxide (1) to afford a quinoxaline 1c andmono-oxide quinoxalines 1a and 1b is described. The experimental conditions werestandardized to the use of two equivalents of amine in ethanol under reflux for two hours,with the aim of studying the distinct reductive profiles of the amines and thechemoselectivity of the process. With the exception of hydrazine hydrate, which reducedcompound 1 to a 3-phenyl-2-quinoxalinecarbohydrazide derivative, the amines only actedas reducing agents. Full article

(This article belongs to the Section Organic Chemistry)

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Open AccessArticle

Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives

by Esther Vicente, Sarah Charnaud, Emily Bongard, Raquel Villar, Asunción Burguete, Beatriz Solano, Saioa Ancizu, Silvia Pérez-Silanes, Ignacio Aldana, Livia Vivas and Antonio Monge

Molecules 2008, 13(1), 69-77; https://doi.org/10.3390/molecules13010069 - 17 Jan 2008

Cited by 40 | Viewed by 13163

Abstract

The aim of this study was to identify new compounds active againstPlasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds weresynthesized and evaluated for antimalarial activity. Eight of them showed an IC₅₀ less than 1 μMagainst [...] Read more.

The aim of this study was to identify new compounds active againstPlasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds weresynthesized and evaluated for antimalarial activity. Eight of them showed an IC₅₀ less than 1 μMagainst the 3D7 strain. Derivative 1 demonstrated high potency (IC₅₀= 0.63 μM) and goodselectivity (SI=10.35), thereby becoming a new lead-compound. Full article

(This article belongs to the Section Organic Chemistry)

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Open AccessReview

Antiparkinson Prodrugs

by Antonio Di Stefano, Piera Sozio and Laura Serafina Cerasa

Molecules 2008, 13(1), 46-68; https://doi.org/10.3390/molecules13010046 - 16 Jan 2008

Cited by 49 | Viewed by 17158

Abstract

Parkinson`s disease (PD) is a progressive, neurodegenerative disorder whichinvolves the loss of dopaminergic neurons of the substantia nigra pars compacta. Currenttherapy is essentially symptomatic, and L-Dopa (LD), the direct precursor of dopamine(DA), is the treatment of choice in more advanced stages of the [...] Read more.

Parkinson`s disease (PD) is a progressive, neurodegenerative disorder whichinvolves the loss of dopaminergic neurons of the substantia nigra pars compacta. Currenttherapy is essentially symptomatic, and L-Dopa (LD), the direct precursor of dopamine(DA), is the treatment of choice in more advanced stages of the disease. Substitutiontherapy with LD is, however, associated with a number of acute problems. The peripheralconversion of LD by amino acid decarboxylase (AADC) to DA is responsible for thetypical gastrointestinal (nausea, emesis) and cardiovascular (arrhythmia, hypotension) sideeffects. To minimize the conversion to DA outside the central nervous system (CNS) LD isusually given in combination with peripheral inhibitors of AADC (carbidopa andbenserazide). In spite of that, other central nervous side effects such as dyskinesia, on-offphenomenon and end-of-dose deterioration still remain. The main factors responsible forthe poor bioavailability and the wide range of inter- and intra-patient variations of plasmalevels are the drug’s physical-chemical properties: low water and lipid solubility, resultingin unfavourable partition, and the high susceptibility to chemical and enzymaticdegradation. In order to improve the bioavailability, the prodrug approach appeared to bethe most promising and some LD prodrugs have been prepared in an effort to solve theseproblems. We report here a review of progress in antiparkinson prodrugs, focusing onchemical structures mainly related to LD, DA and dopaminergic agonists. Full article

(This article belongs to the Section Medicinal Chemistry)

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Open AccessCommunication

A New Phenolic Amide from the Roots of Paris verticillata

by Kyu Ha Lee, Min Cheol Yang, Ki Hyun Kim, Hak Cheol Kwon, Sang Un Choi and Kang Ro Lee

Molecules 2008, 13(1), 41-45; https://doi.org/10.3390/molecules13010041 - 16 Jan 2008

Cited by 25 | Viewed by 10422

Abstract

A new phenolic amide 8, together with the nine known phenolic compounds 1-7,9 and 10 were isolated from the MeOH extract of the roots of Paris verticillata. Thestructure of the new compound 8 was determined to be 1-N-feruloylaminobutyl-4-ρ-hydroxybenzamide by spectroscopic methods. The isolated [...] Read more.

A new phenolic amide 8, together with the nine known phenolic compounds 1-7,9 and 10 were isolated from the MeOH extract of the roots of Paris verticillata. Thestructure of the new compound 8 was determined to be 1-N-feruloylaminobutyl-4-ρ-hydroxybenzamide by spectroscopic methods. The isolated compounds were tested forcytotoxicity against four human tumor cell lines using the SRB assay. Full article

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Open AccessArticle

Efficacy of DA-7218, a New Oxazolidinone Prodrug, in the Treatment of Experimental Actinomycetoma Produced by Nocardia brasiliensis

by Nelly Alejandra Espinoza-González, Oliverio Welsh, Noemi Waksman De Torres, Norma Cavazos-Rocha, Jorge Ocampo-Candiani, Salvador Said-Fernandez, Gerardo Lozano-Garza, Sung-Hak Choi and Lucio Vera-Cabrera

Molecules 2008, 13(1), 31-40; https://doi.org/10.3390/molecules13010031 - 11 Jan 2008

Cited by 21 | Viewed by 11953

Abstract

Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and itscorresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-2-oxo-5-oxazolidinyl) methyl disodium phosphate (DA-7218), have shown very goodactivity against several Gram positive bacteria, including Nocardia and Mycobacterium. Inthe present work we evaluated the therapeutic in vivo effects of DA-7218 on Nocardiabrasiliensis. We first [...] Read more.

Two recently synthesized oxazolidinones: (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyloxazolidin-2-one (DA-7157) and itscorresponding pro-drug (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-2-oxo-5-oxazolidinyl) methyl disodium phosphate (DA-7218), have shown very goodactivity against several Gram positive bacteria, including Nocardia and Mycobacterium. Inthe present work we evaluated the therapeutic in vivo effects of DA-7218 on Nocardiabrasiliensis. We first determined the plasma concentration of the prodrug in BALB/c miceusing several doses and then tested its activity in an in vivo experimental actinomycetomamurine model. At the end of treatment, there was a statistically significant differencebetween the three drug receiving groups (25, 12.5 and 5 mg/kg) and the control group(saline solution) (p=0.001), proving that DA-7218 is effective for the treatment of experimental murine actinomycetoma. This compound could be a potential option forpatients affected with mycetoma by Nocardia brasiliensis. Full article

(This article belongs to the Section Medicinal Chemistry)

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Open AccessArticle

Design and Synthesis of Novel N-Benzylidenesulfonohydrazide Inhibitors of MurC and MurD as Potential Antibacterial Agents

by Rok Frlan, Andreja Kovač, Didier Blanot, Stanislav Gobec, Slavko Pečar and Aleš Obreza

Molecules 2008, 13(1), 11-30; https://doi.org/10.3390/molecules13010011 - 11 Jan 2008

Cited by 36 | Viewed by 9408

Abstract

A series of novel N-benzylidenesulfonohydrazide compounds were designedand synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) andUDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved inthe biosynthesis of bacterial cell-walls. Some compounds possessed inhibitory activityagainst both enzymes with IC₅₀ values as low as 30 [...] Read more.

A series of novel N-benzylidenesulfonohydrazide compounds were designedand synthesized as inhibitors of UDP-N-acetylmuramic acid:L-alanine ligase (MurC) andUDP-N-acetylmuramoyl-L-alanine:D-glutamate ligase (MurD) from E. coli, involved inthe biosynthesis of bacterial cell-walls. Some compounds possessed inhibitory activityagainst both enzymes with IC₅₀ values as low as 30 μM. In addition, a new, one-potsynthesis of amidobenzaldehydes is reported. Full article

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Open AccessCommunication

NMR Spectra of Sparteine N1-oxide and α-Isosparteine N-oxide

by Beata Jasiewicz

Molecules 2008, 13(1), 3-10; https://doi.org/10.3390/molecules13010003 - 9 Jan 2008

Cited by 6 | Viewed by 8187

Abstract

Sparteine N1-oxide and α-isosparteine N-oxide were prepared and theirstructures determined for the first time by ¹H- and ¹³C-NMR spectroscopy using twodimensionaltechniques. The N-oxide effects were also calculated. Full article

(This article belongs to the Special Issue Alkaloids: Novel Therapeutic Perspectives)

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Open AccessEditorial

2007 – An Excellent Year for Molecules and a Look Forward to 2008

by Derek McPhee and Shu-Kun Lin

Molecules 2008, 13(1), 1-2; https://doi.org/10.3390/molecules13010001 - 9 Jan 2008

Cited by 1 | Viewed by 4890

Abstract

As already anticipated in August 2007 [1], the year that just concluded proved to be a truly outstanding one for MDPI's flagship journal Molecules.[...] Full article

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Molecules, Volume 13, Issue 1 (January 2008) – 19 articles , Pages 1-203

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