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Discovery of N-benzyl-N′-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): Modification of the acyl portion

✍ Scribed by Maosheng Duan; Jennifer Peckham; Mark Edelstein; Robert Ferris; Wieslaw M. Kazmierski; Andrew Spaltenstein; Pat Wheelan; Zhiping Xiong

Book ID: 104005004
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 255 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.10.042

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✦ Synopsis

Modification of the acyl moiety in the CCR5 lead molecule 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationship (SAR) derived from these studies further guided the optimization efforts, ultimately leading to the discovery of 36 with an acceptable drug-like profile.

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