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Synthesis of combinatorial libraries of vinylogous sulfonopeptides


In the context of isosteric replacement of the peptide bond it seems very interesting to synthesize pseudopeptides characterized by the presence of sulfonamide bond. This modification gives important properties to sulfonamidopeptides and makes them pro- mising candidates in the development of protease inhibitors and new drugs. The development of a combinatorial library of viny- logous sulfonopeptides will be specially interesting due to its great pharmaceutical potential. The aim of this project is to synthesize vinylogous sulfonopep- tides and combinatorial libraries with them. It includes three steps:
a) Synthesis of the functionalized monomers (vinylogous a- minosulfonic acids) like the derivatives of Ser. Thr, Asn, Gln, Lys, Met, Trp. b) Optimization of the coupling yields of the monomers and the development of solid phase synthesis method.
c) Combinatorial library synthesis both on solid support and in solution. Part of the solid supported combinatorial library will be sponsored by "Pharmacia" (the Swedish-Italian Multinational Pharmaceutical Company). This Multinational will also test the sulfonopeptide libraries for biological and pharmacological activity.

Funding Scheme

RGI - Research grants (individual fellowships)


Via Venezian 21
20133 Milano

Participants (1)

Not available