Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the-ligands

…, S Kay, DE Walters, Y Koh, K Maeda, H Mitsuya

Index: Ghosh, Arun K.; Schiltz, Gary; Perali, Ramu Sridhar; Leshchenko, Sofiya; Kay, Stephanie; Walters, D. Eric; Koh, Yasuhiro; Maeda, Kenji; Mitsuya, Hiroaki Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1869 - 1873

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Citation Number: 48

Abstract

A series of novel oxyindole-derived HIV-1 protease inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 2 (TMC-114) bound to HIV-1 protease. The effects of substituents, spirocyclic rings, and ring sizes have been ...