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Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators.

Authors :
Sugama H
Matsudaira T
Yanagisawa H
Ohashi R
Nawano M
Yasuda K
Takayama H
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Aug 01; Vol. 30 (15), pp. 127249. Date of Electronic Publication: 2020 May 06.
Publication Year :
2020

Abstract

This paper presents the synthesis and glucokinase activity of novel hydrazone derivatives. The 2-(4-cyclopropylsulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-acetamide derivatives 5a-5h presented the in vitro glucokinase activities and in vivo blood glucose-lowering effects in mice. Particularly, 5h showed an oral hypoglycemic effect in rats at 1 mg/kg. These hydrazone derivatives are a potential new class of glucokinase activators for the treatment of type 2 diabetes.<br />Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.<br /> (Copyright © 2020 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
30
Issue :
15
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
32527453
Full Text :
https://doi.org/10.1016/j.bmcl.2020.127249