Synthesis of amino acid derivatives of benzofuroxan

Abstract

149 Furoxans (derivatives of 1,2,5 oxadiazole N oxide) are heterocyclic thermally stable compounds. Furoxans can slowly produce NO for a long time and do not cause devel opment of nitrate tolerance [1]. In the design of hybrid pharmaceuticals, they are often introduced as an NO producing fragment into the molecule of a known prepa ration to impart it with, for example, cGMP dependent vasodilation or antiaggregatory properties [1–3]. One of the recent directions in medicinal chemis try is the design of hybrid multifunctional pharmaceu ticals that combine two or more pharmacophores in one molecule. The wide spectrum of pharmacological activity of these pharmaceuticals, the ability of drug to interact with several targets, is matched against selectivity. Amino acids are often used as an addi tional pharmacophore [4]. Amino acids can behave as both independent pharmacophores and linkers for the attachment of an additional pharmacologically active fragment due to the presence of a free carboxyl group.