CCR5 antagonists may be effective as anti-HIV-1 agents

"We have previously reported the novel lead compound 1a as a CCR5 antagonist for treatment of HIV-1 infection," wrote researchers in Japan.

"SAR studies on incorporating various acyl groups as a replacement for the 5-oxopyrrolidine-3-carbonyl group of the lead structure resulted in the discovery of N-[3-(4-benzylpiperidin-1-yl)propyl]-N,N-1-diphenylurea (4a) with significantly improved CCR5 binding affinity. Substitutions (4-Cl, 4e,f; 4-Me, 4i) on the N'-phenyl ring further increased the binding affinity," S. Imamura and coauthors reported.

"Introduction of polar substituents...

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