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ID: ALA1149644

Journal: Bioorg Med Chem Lett

Title: alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists.

Authors: Sisto A, Altamura M, Cardinali F, D'Andrea P, Rossi C, Fattori D.

Abstract: MEN 15596 is a small molecule, potent and selective antagonist of NK(2) receptor, possessing high affinity and potency at the guinea-pig and human receptors whose pharmacological characterization has been recently published. Here we report how the corresponding class of compounds was derived from a tri-peptide library and the first optimization round to improve both in vitro activity and physicochemical properties.

CiteXplore: 17604625

DOI: 10.1016/j.bmcl.2007.06.053