Preparation and structure-activity relationship of novel P1/P1'-substituted cyclic urea-based human immunodeficiency virus type-1 protease inhibitors

DA Nugiel, K Jacobs, T Worley, M Patel…

Index: Nugiel; Jacobs; Worley; Patel; Kaltenbach III; Meyer; Jadhav; De Lucca; Smyser; Klabe; Bacheler; Rayner; Seitz Journal of Medicinal Chemistry, 1996 , vol. 39, # 11 p. 2156 - 2169

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Citation Number: 117

Abstract

A series of novel P1/P1'-substituted cyclic urea-based HIV-1 protease inhibitors was prepared. Three different synthetic schemes were used to assemble these compounds. The first approach uses amino acid-based starting materials and was originally used to prepare DMP 323. The other two approaches use l-tartaric acid or l-mannitol as the starting material. The required four contiguous R, S, S, R centers of the cyclic urea scaffold are introduced ...