Journal
CHEMMEDCHEM
Volume 3, Issue 11, Pages 1756-1762Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.200800183
Keywords
AIDS; antiviral agents; aryloxy imidazole; medicinal chemistry; NNRTI
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A major problem associated with non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of HIV is their vulnerability to mutations in the allosteric binding site of reverse transcriptase that can result in the development of a resistant virus. Herein we present the optimization of a series of 5-aryloxy imidazoles, which possess a balanced pharmacological profile against both wild-type enzyme and the clinically relevant mutations K103N and Y181C Subtle structural changes were used to probe structure-activity relationships relating to both potency and metabolic stability, which led to an imidazole derivative with an impressive overall profile.
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