Design, synthesis and biological evaluation of 3-substituted 2, 5-dimethyl-N-(3-(1H-tetrazol-5-yl) phenyl) pyrroles as novel potential HIV-1 gp41 inhibitors

XY He, P Zou, J Qiu, L Hou, S Jiang, S Liu…

Index: He, Xiao-Yang; Zou, Peng; Qiu, Jiayin; Hou, Ling; Jiang, Shibo; Liu, Shuwen; Xie, Lan Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 22 p. 6726 - 6734

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Citation Number: 20

Abstract

Based on the structure of HIV-1 gp41 binding site for small-molecule inhibitors, optimization of lead 2 resulted in the discovery of a new series of 2, 5-dimethyl-3-(5-(N-phenylrhodaninyl) methylene)-N-(3-(1H-tetrazol-5-yl) phenyl) pyrrole compounds with improved anti-HIV-1 activity. The most active compounds 13a and 13j exhibited significant potency against gp41 6-HB formation with IC50 values of 4.4 and 4.6 μM and against HIV-1 replication in the MT ...