| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10595140 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
Non-nucleoside inhibitors of HIV-1 reverse transcriptase are reported that have ca. 100-fold greater solubility than the structurally related drugs etravirine and rilpivirine, while retaining high anti-viral activity. The solubility enhancements come from strategic placement of a morpholinylalkoxy substituent in the entrance channel of the NNRTI binding site. Compound 4d shows low-nanomolar activity similar to etravirine towards wild-type HIV-1 and key viral variants.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mariela Bollini, José A. Cisneros, Krasimir A. Spasov, Karen S. Anderson, William L. Jorgensen,