期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 19, 页码 5909-5912出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.081
关键词
Integrase; Inhibitor; Metal chelator; Synthesis
Synthesis of a diverse set of azoles and their utilizations as an amide isostere in the design of HIV integrase inhibitors is described. The Letter identified thiazole, oxazole, and imidazole as the most promising heterocycles. Initial SAR studies indicated that these novel series of integrase inhibitors are amenable to lead optimization. Several compounds with low nanomolar inhibitory potency are reported. (C) 2010 Elsevier Ltd. All rights reserved.
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