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Get Free AccessNon-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that incorporate a 7-indolizinylamino or 2-naphthylamino substituent on a pyrimidine or 1,3,5-triazine core. The most potent compounds show below 10 nanomolar activity towards wild-type HIV-1 and variants bearing Tyr181Cys and Lys103Asn/Tyr181Cys resistance mutations. The compounds also feature good aqueous solubility. Crystal structures for two complexes enhance the analysis of the structure–activity data.
Won-Gil Lee, Kathleen M. Frey, Ricardo Gallardo‐Macias, Krasimir A. Spasov, Albert H. Chan, Karen S. Anderson, William L. Jorgensen (2015). Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase. Bioorganic & Medicinal Chemistry Letters, 25(21), pp. 4824-4827, DOI: 10.1016/j.bmcl.2015.06.074.
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Type
Article
Year
2015
Authors
7
Datasets
0
Total Files
0
Language
English
Journal
Bioorganic & Medicinal Chemistry Letters
DOI
10.1016/j.bmcl.2015.06.074
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