Antileishmanial activity screening of 5-nitro-2-heterocyclic benzylidene hydrazides

…, MA Avery, BL Tekwani, SI Khan, EI Ferreira

文献索引：Rando, Daniela G.; Avery, Mitchell A.; Tekwani, Babu L.; Khan, Shabana I.; Ferreira, Elizabeth I. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6724 - 6731

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被引用次数: 32

摘要

A series of 53 nitro derivatives rationally designed were obtained by parallel synthesis and screened against Leishmania donovani. Six compounds exhibited IC50 values lower than standard drugs. Brief SAR analysis revealed that substitution is important to the activity. Nitrothiophene analogues were more potent than the nitrofuran ones. This was attributed to the ability of sulfur atoms in accommodating electrons from nitro group, which facilitate its ...