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Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.

Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.
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Zhao Y, Gu Q, Morris-Natschke SL, Chen CH, Lee KH,


Zhao Y, Gu Q, Morris-Natschke SL, Chen CH, Lee KH, (click to view)

Zhao Y, Gu Q, Morris-Natschke SL, Chen CH, Lee KH,

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Journal of medicinal chemistry 2016 Sep 2259(19) 9262-9268

Abstract

Two "privileged fragments", caffeic acid and piperazine, were integrated into bevirimat producing new derivatives with improved activity against HIV-1/NL4-3 and NL4-3/V370A carrying the most prevalent bevirimat-resistant polymorphism. The activity of one of these, 18c, was increased by 3-fold against NL4-3 and 51-fold against NL4-3/V370A. Moreover, 18c is a maturation inhibitor with improved metabolic stability. Our study suggested that integration of privileged motifs into promising natural product skeletons is an effective strategy for discovering potent derivatives.

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