Correlation of anti-HIV activity with anion spacing in a series of cosalane analogues with extended polycarboxylate pharmacophores

…, C Pannecouque, M Witvrouw, TL Loftus…

Index: Santhosh; Paul; De Clercq; Pannecouque; Witvrouw; Loftus; Turpin; Buckheit, Jr.; Cushman Journal of Medicinal Chemistry, 2001 , vol. 44, # 5 p. 703 - 714

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Citation Number: 36

Abstract

Cosalane and its synthetic derivatives inhibit the binding of gp120 to CD4 as well as the fusion of the viral envelope with the cell membrane. The binding of the cosalanes to CD4 is proposed to involve ionic interactions of the negatively charged carboxylates of the ligands with positively charged arginine and lysine amino acid side chains of the protein. To investigate the effect of anion spacing on anti-HIV activity in the cosalane system, a series ...