The development of cyclic sulfolanes as novel and high-affinity P2 ligands for HIV-1 protease inhibitors

…, HY Lee, WJ Thompson, C Culberson…

Index: Ghosh, Arun K.; Lee, Hee Yoon; Thompson, Wayne J.; Culberson, Chris; Holloway, M. Katharine; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 8 p. 1177 - 1188

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Citation Number: 58

Abstract

Design and synthesis of a novel series of protease inhibitors incorporating conformationally constrained cyclic ligands for the &-substrate binding site of HIV-1 protease is described. We recently reported urethanes of 3-tetrahydrofuranyl as PZ ligands for HIV-1 protease inhibitors. Subsequently, we have found that the urethane of 3 (S)-hydroxysulfolane further increased the in uitro potency of these inhibitors. Furthermore, introduction of a small 2- ...