Article
Heterocycle amide isosteres: An approach to overcoming resistance for HIV-1 integrase strand transfer inhibitors.
Bioorganic & medicinal chemistry letters - 1 Feb 2020
Peese Kevin M, Naidu B Narasimhulu, Patel Manoj, Li Chen, Langley David R, Terry Brian, Protack Tricia, Gali Volodymyr, Lin Zeyu, Samanta Himadri K, Zheng Ming, Jenkins Susan, Dicker Ira B, Krystal Mark R, Meanwell Nicholas A, Walker Michael A
Abstract excerpt
A series of heterocyclic pyrimidinedione-based HIV-1 integrase inhibitors was prepared and screened for activity against purified integrase enzyme and/or viruses modified with the following mutations within integrase: Q148R, Q148H/G140S and N155H. These are mutations that result in resistance to the first generation integrase inhibitors raltegravir and elvitegravir. Based on consideration of drug-target...
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