Article
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
Journal of medicinal chemistry - 26 Feb 2009
Jones Lyn H, Allan Gill, Barba Oscar, Burt Catherine, Corbau Romuald, Dupont Thomas, Knöchel Thorsten, Irving Steve, Middleton Donald S, Mowbray Charles E, Perros Manos, Ringrose Heather, Swain Nigel A, Webster Robert, Westby Mike, Phillips Chris
Abstract excerpt
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...
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