期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 3, 页码 917-922出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.070
关键词
Non-nucleoside reverse transcriptase; HIV; Triazolinone; Pyridone; Inhibitor
The optimization of a novel series of non-nucleoside reverse transcriptase inhibitors (NNRTI) led to the identification of pyridone 36. In cell cultures, this new NNRTI shows a superior potency profile against a range of wild type and clinically relevant, resistant mutant HIV viruses. The overall favorable preclinical pharmacokinetic profile of 36 led to the prediction of a once daily low dose regimen in human. NNRTI 36, now known as MK-1439, is currently in clinical development for the treatment of HIV infection. (C) 2013 Elsevier Ltd. All rights reserved.
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