Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 4, Pages 1219-1223Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801322h
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A major problem associated with non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of HIV is their lack of resilience to mutations in the reverse transcriptase (RT) enzyme. Using structural overlays of the known inhibitors efavirenz and capravirine complexed in RT as a starting point, and structure-based drug design techniques, we have created a novel series of indazole NNRTIs that possess excellent metabolic stability and mutant resilience.
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