期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 18, 页码 5213-5216出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.091
关键词
Anti-HIV agent; NNRTI; Drug solubility
资金
- National Institutes of Health [AI44616, GM32136, GM49551]
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. (C) 2013 Elsevier Ltd. All rights reserved.
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