In vivo biological activity of antioxidative aminothiazole derivatives

Chemical & Pharmaceutical Bulletin
O UchikawaT Doi

Abstract

For the development of novel antioxidants having therapeutic utility, a new series of condensed 4- and 5-aminothiazole derivatives has been synthesized using simple methods. Condensed 4-aminothiazoles were prepared by the reaction of alpha-bromolactams with thioamides in ethanol and 5-aminothiazole derivatives were obtained by the treatment of 3-(acylamino)lactams with a thiating agent such as phosphorous pentasulfide and Lawesson's reagent in pyridine. In vitro assay of the condensed 5-aminothiazole derivatives showed them to be potent inhibitors of lipid peroxidation. In order to evaluate these compounds in an in vivo system, we devised a simple and reproducible method in which the inhibition of characteristic behaviors induced by spinal injection of FeCl2 was expressed numerically. Compounds having strong in vitro activity protected the central nervous system form injury caused by iron-dependent lipid peroxidation. The results suggest that the in vivo assay developed in this study should be useful as a screening method for antioxidants and also that condensed 5-aminothiazole derivatives are promising candidates for the treatment of traumatic and ischemic injury of the central nervous system.

Citations

May 10, 2008·Chemico-biological Interactions·Strayo DeT P A Devasagayam
Nov 7, 2012·Environmental Toxicology and Pharmacology·K B KalpanaVenugopal P Menon
Oct 16, 2004·Fundamental & Clinical Pharmacology·Aruna KodeVenugopal P Menon
Jan 1, 2007·Toxicology Mechanisms and Methods·Aruna KodeVenugopal P Menon
Sep 18, 2007·Chemical Reviews·Turan OzturkOlcay Mert
May 1, 2010·Chemical Reviews·Turan OzturkOlcay Mert
Mar 14, 2013·ACS Medicinal Chemistry Letters·Luigi MessoriDavide Franceschini
Jan 9, 2003·Chemical Reviews·Tadeusz S Jagodziński

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