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.
Original language | English |
---|---|
Pages (from-to) | 5909-5912 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 20 |
Issue number | 19 |
DOIs | |
Publication status | Published - 1 Oct 2010 |
Externally published | Yes |
Keywords
- Inhibitor
- Integrase
- Metal chelator
- Synthesis