Segregation of Activity Profile in Benzimidazoles: Effect of Spacers at 5(6)-Position of Methyl Benzimidazole-2-carbamates [1]
| Autor: | Satyavan Sharma, Amiya P. Bhaduri, J. C. Katiyar, R. K. Chatterjee, Shiv K. Agarwal |
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| Rok vydání: | 1993 |
| Předmět: | |
| Zdroj: | Zeitschrift für Naturforschung C. 48:829-838 |
| ISSN: | 1865-7125 0939-5075 |
| Popis: | 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(6)-position of benzimidazole-2-carbamate, on the activity against Ancylostoma ceylanicum (hookworm), Syphacia obvelata (pinworm), Hymenolepis nana (tapeworm), Litomosoides carinii and Acanthocheilonema viteae (filarial worm) has been presented. This analysis indicates that for activity against intestinal helminth the presence of one spacer holding the pharmacophore approximately 3 Å apart from the parent nucleus is usually preferred. While for activity against tissue dwelling parasite, the repetition of the benzimidazole-2-carbamate nucleus joined together through the 5,5′-position with one spacer kept apart by distance of 3 Å unit is usually desired. |
| Databáze: | OpenAIRE |
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