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Studies on the structure–activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents

✍ Scribed by Li Ben; Eric Dale Jones; Enkun Zhou; Chen Li; Dean Cameron Baylis; Shanghai Yu; Miao Wang; Xing He; Jonathan Alan Victor Coates; David Ian Rhodes; Gang Pei; John Joseph Deadman; Xin Xie; Dawei Ma

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 524 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.05.102

No coin nor oath required. For personal study only.

✦ Synopsis

A novel series of CCR5 antagonists has been identified, utilizing the lead, nifeviroc, which were further modified based on bioisosteric principles. Lead optimization was pursued by balancing potential toxicity and potency. Potent analogues with low toxic properties were successfully developed by formation of urea and amide bonds at the nitrogen at position 4-of the pyrrolidine ring.

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