期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 24, 页码 7512-7517出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.10.034
关键词
HIV-1; Capsid assembly inhibitor; Benzimidazole; X-ray crystal structure
A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved the antiviral potency by a factor of 1000. The X-ray structure of 33 complexed with the capsid N-terminal domain allowed identification of major interactions between the inhibitor and the protein. (C) 2012 Elsevier Ltd. All rights reserved.
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