Identification of optimal anion spacing for anti-HIV activity in a series of cosalane tetracarboxylates |
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Authors: | Paul G C De Clercq E Pannecouque C Witvrouw M Loftus T L Turpin J A Buckheit R W Cushman M |
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Affiliation: | Department of Medicinal Chemistry and Molecular Pharmacology, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, IN 47907, USA. |
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Abstract: | The binding of the anti-HIV agent cosalane to CD4 is thought to involve ionic interactions of negatively charged carboxylates of the ligand with positively charged residues on the surface of the protein. An investigation of the optimal anion distances for anti-HIV activity in a series of cosalane tetracarboxylate analogues has been completed, and maximal activity results when the two proximal and the two distal carboxylates are separated by eight atoms. |
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