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Cycloalkylpyranones and cycloalkyldihydropyrones as HIV protease inhibitors: exploring the impact of ring size on structure-activity relationships

…, DJ Anderson, JW Strohbach, SR Turner…

文献索引:Romines, Karen R.; Morris, Jeanette K.; Howe, W. Jeffrey; Tomich, Paul K.; Horng, Miao-Miao; Chong, Kong-Teck; Hinshaw, Roger R.; Anderson, David J.; Strohbach, Joseph W.; Turner, Steve-R.; Mizsak, Steve A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 20 p. 4125 - 4130

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被引用次数: 65

摘要

Previously, 3-substituted cycloalkylpyranones, such as 2d, have proven to be effective inhibitors of HIV protease. In an initial series of 3-(1-phenylpropyl) derivatives with various cycloalkyl ring sizes, the cyclooctyl analog was the most potent. We became interested in exploring the influence of other structural changes, such as substitution on the phenyl ring and saturation of the 5, 6-double bond, on the cycloalkyl ring size structure-activity ...