Small molecule fusion inhibitors: design, synthesis and biological evaluation of (Z)-3-(5-(3-benzyl-4-oxo-2-thioxothiazolidinylidene) methyl)-N-(3-carboxy-4-hydroxy) …

…, L Lu, J Qiu, P Zou, F Yu, XK Jiang, L Li, S Jiang…

Index: He, Xiao-Yang; Lu, Lu; Qiu, Jiayin; Zou, Peng; Yu, Fei; Jiang, Xing-Kai; Li, Lin; Jiang, Shibo; Liu, Shuwen; Xie, Lan Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 23 p. 7539 - 7548

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Citation Number: 8

Abstract

Abstract By a scaffold elongation strategy, a series of (Z)-3-(5-(3-benzyl-4-oxo-2- thioxothiazolidinylidene) methyl)-N-(3-carboxy-4-hydroxy) phenyl-2, 5-dimethylpyrroles and related derivatives with a linear multi-aromatic-ring skeleton were designed, synthesized, and evaluated in HIV-1 gp41 and cellular assays. Among them, the most active compounds, 12e, 12g, and 12k with a one-carbon linker (n= 1) between the rhodanine (C) and phenyl ( ...