Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 19, Pages 9262-9268Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00461
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- National Institute of Allergy and Infectious Diseases (NIAID) [AI-033066]
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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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