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Pharmacophore-based design, synthesis, and biological evaluation of novel chloro-pyridazine piperazines as human rhinovirus (HRV-3) inhibitors

✍ Scribed by Hongliang Wang; Junhai Xiao; Dapeng Gao; Xian Zhang; Hui Yan; Zehui Gong; Tinmin Sun; Song Li

Publisher: Elsevier Science
Year: 2011
Tongue: English
Weight: 512 KB
Volume: 21
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.12.001

No coin nor oath required. For personal study only.

✦ Synopsis

A series of chloro-pyridazine piperazines were developed based on the structure of human rhinovirus (HRV) capsid-binding inhibitors with proven activity using a pharmacophore model. A preliminary evaluation demonstrated potent activity against HRV-3 with low cytotoxicity. A docking analysis indicated that 8a could fit into, and form tight interactions (e.g., H-bonds, σ-π effect) with the active site in VP1.

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