Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase

…, RT Nolte, L Wang, RG Ferris, M Edelstein…

Index: Chong, Pek; Sebahar, Paul; Youngman, Michael; Garrido, Dulce; Zhang, Huichang; Stewart, Eugene L.; Nolte, Robert T.; Wang, Liping; Ferris, Robert G.; Edelstein, Mark; Weaver, Kurt; Mathis, Amanda; Peat, Andrew Journal of Medicinal Chemistry, 2012 , vol. 55, # 23 p. 10601 - 10609

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Citation Number: 30

Abstract

A new series of non-nucleoside reverse transcriptase inhibitors based on an imidazole- amide biarylether scaffold has been identified and shown to possess potent antiviral activity against HIV-1, including the NNRTI-resistant Y188L mutated virus. X-ray crystallography of inhibitors bound to reverse transcriptase, including a structure of the Y188L RT protein, was used extensively to help identify and optimize the key hydrogen-bonding motif. This led ...