期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 52, 期 4, 页码 1219-1223出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm801322h
关键词
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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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