Synthesis, biological evaluation and 3D-QSAR studies of 3-keto salicylic acid chalcones and related amides as novel HIV-1 integrase inhibitors

…, S Patil, TW Sanchez, N Neamati, RF Schinazi…

Index: Sharma, Horrick; Patil, Shivaputra; Sanchez, Tino W.; Neamati, Nouri; Schinazi, Raymond F.; Buolamwini, John K. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 6 p. 2030 - 2045

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Citation Number: 52

Abstract

HIV-1 integrase is one of the three most important enzymes required for viral replication and is therefore an attractive target for anti retroviral therapy. We herein report the design and synthesis of 3-keto salicylic acid chalcone derivatives as novel HIV-1 integrase inhibitors. The most active compound, 5-bromo-2-hydroxy-3-[3-(2, 3, 6-trichlorophenyl) acryloyl] benzoic acid (25) was selectively active against integrase strand transfer, with an IC50 of ...