Synthesis of 2-Substituted Benzimidazole-5-carbamates as Potential Antifilarial Agents
نویسنده
چکیده
A large group of benzimidazole derivatives are highly effective as an anthelmintics [ 11. Among these, mebendazole (la, methyl 5-benzoylbenzimidazole-2-carbamate) and flubendazole (lb, methyl 5-p-fluorobenzoylbenzimidazole-Z-carbamate) have demonstrated a broad-spectrum of activity against helminth diseases including filarial infections [2-51. In our continuing studies to develop new antifilarial agents [6-81, we have found that two of the metabolites of mebendazole, methyl 5-(c~-hydroxylbenzyl)benzimidazole-2-carbamate (lc), and, methyl 5-benzylbenzimidazole-2-carbamate (la) possess antifilarial activity very similar to that of the parent drug l a [9]. Recently, a series of benzothiazoles, typified by structure 2, were
منابع مشابه
Synthesis, Characterization and Evaluation of Novel 6- Substituted Benzimidazole-2-carbamates as Potential Antimicrobial Agents
Objective: The aim of the present work was to synthesize and characterize a series of 6substituted benzimidazole-2-carbamic acid derivatives and evaluate them for antimicrobial activity. Methods: A novel series of 6-substituted benzimidazole-2-carbamic acid derivatives (6a-f) were synthesized by reacting substituted benzyl chlorides (2a-c) with 4-hydroxy -2nitro aniline (3) in the presence of a...
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The design and synthesis o f a series o f alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), l,2-dimethyl-3-methoxycarbonyl-4,5-disubstituted pyrroles (17—19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydropyrimidine (24) have been carried out ...
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The design and synthesis of a series of alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), 1,2-dimethyl-3-methoxy-carbonyl-4,5-disubstituted pyrroles (17-19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydro-pyrimidine (24) have been carried out ...
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The design and synthesis of a series of methyl 5(6)-substituted benzimidazole-2-carbamates as possible anthelmintics have been described. A rational analysis of the structural parameters which segregate the activity of resulting benzimidazole-2-carbamates against enteric and tissue dwelling helminths is presented. The influence of single and multiple spacers, which link the pharmacophores at 5(...
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A water soluble, Bronsted acid, 5-sulfosalicylic acid as an efficient organocatalyst was used for the synthesis of physiologically active 2-substituted benzimidazole derivatives from o-phenylenediamine and aromatic aldehydes in ethanol at reflux condition. Cost-effectiveness, use of non-hazardous solvents, metal free and commercially available catalyst, single-step, environmentally fri...
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