320727-73-9Relevant academic research and scientific papers
Diacylhydrazine derivatives
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Page/Page column 22; 23, (2008/06/13)
Diacylhydrazine derivatives of general formula (I) wherein X, Y, Z, R1,2and R3are as defined herein, and their physiologically acceptable salts or solvates thereof, are integrin inhibitors and can be used to combat thromboses, myocardial infarcts, coronary cardiac diseases, arteriosclerosis, inflammations, tumors, osteoporosis, infections, and restenosis following angioplasty or during pathological processes that are maintained or propagated by angiogenesis.
Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists
Sulyok,Gibson,Goodman,H?lzemann,Wiesner,Kessler
, p. 1938 - 1950 (2007/10/03)
The solid-phase synthesis of a low molecular weight RGD mimetic library is described. Activities of the compounds in inhibiting the interaction of ligands, vitronectin and fibrinogen, with isolated immobilized integrins αvβ3 and αIIbβ3 were determined in a screening assay. Highly active and selective nonpeptide αvβ3 integrin antagonists with regard to orally bioavailability were developed, based on the aza-glycine containing lead compound 1. An important variation is the substitution of the aspartic amide of 1 by an aromatic residue. Furthermore, different guanidine mimetics have been incorporated to improve the pharmacokinetic profile. Exchange of the β-amino acid NH by a methylene moiety in one set of RGD mimetics leads to the azacarba analogue compounds representing a novel peptidomimetic approach, which should increase the metabolic stability.
