PMID: 6540312Aug 1, 1984Paper

Syntheses and anthelmintic activity of alkyl 5(6)-(substituted-carbamoyl)- and 5(6)-(disubstituted-carbamoyl)benzimidazole-2-carbamates and related compounds

Journal of Medicinal Chemistry
S KumarA B Sen

Abstract

A number of alkyl 5(6)-(substituted-carbamoyl)- and 5(6)-(disubstituted-carbamoyl)benzimidazole-2-carbamates and related compounds have been synthesized, and their anthelmintic activity against various intestinal helminths of experimental animals have been evaluated. A large percentage of the compounds synthesized showed noteworthy activity against Ancylostoma ceylanicum and at higher doses against Hymenolepsis nana infections. Compared to the alkyl 5(6)-(substituted-carbamoyl)benzimidazole-2-carbamates, the disubstituted carbamoyl analogues were found to exhibit better anthelmintic activity. The most active compound of the series, namely, methyl 5(6)-[(N-2-pyridylpiperazino)carbamoyl]benzimidazole-2-carbamate (90), has been screened against intestinal helminths in higher animals and as a micro- and macrofilaricidal agent. Compound 90 has been identified as a broad-spectrum anthelmintic agent. Compound 90 has been identified as a broad-spectrum anthelmintic in view of its efficacy against A. ceylanicum (hamsters and dogs), H. nana (rats), Nippostrongylus brasiliensis (rats), Syphacia obvelata (mice), A. tubaeformis (cat), Toxocara spp. (cat), and Litomosoides carinii (cotton rat).

Citations

Nov 1, 1991·Medicinal Research Reviews·S K Singh, S Sharma
Feb 5, 2004·Bioorganic & Medicinal Chemistry·Marco MorPier Vincenzo Plazzi
Jul 31, 1999·Bioorganic & Medicinal Chemistry·S K SrivastavaR K Chatterjee
Jul 18, 2006·Parasite Immunology·R T FujiwaraS Mendez
Nov 25, 2000·The Journal of Pharmacy and Pharmacology·N V NagarajaR C Gupta
Feb 1, 1992·Annals of Tropical Medicine and Parasitology·S GuptaS C Maitra
May 7, 1999·Journal of Medicinal Chemistry·S K SrivastavaR K Chatterjee

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