Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363008 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
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.
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Related Topics
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Organic Chemistry
Authors
Giang Le, Nick Vandegraaff, David I. Rhodes, Eric D. Jones, Jonathan A.V. Coates, Neeranat Thienthong, Lisa J. Winfield, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J. Deadman,