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Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.


ABSTRACT: A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported further optimization.

SUBMITTER: Feng S 

PROVIDER: S-EPMC4416423 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.

Feng Song S   Hong Di D   Wang Baoxia B   Zheng Xiufang X   Miao Kun K   Wang Lisha L   Yun Hongying H   Gao Lu L   Zhao Shuhai S   Shen Hong C HC  

ACS medicinal chemistry letters 20150125 3


A series of imidazolepyridine derivatives were designed and synthesized according to the established docking studies. The imidazopyridine derivatives were found to have good potency and physical-chemical properties. Several highly potent compounds such as 8ji, 8jl, and 8jm were identified with single nanomolar activities. The most potent compound 8jm showed an IC50 of 3 nM, lower microsome clearance and no CYP inhibition. The profile of 8jm appeared to be superior to BMS433771, and supported fur  ...[more]

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