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

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ID: 108593
2020
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Ranked #63 of 246 articles by views in Bioorganic & medicinal chemistry letters

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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.
Reference Key
sugama2020designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Sugama, Hiroshi;Matsudaira, Tetsuji;Yanagisawa, Hideyuki;Ohashi, Rikiya;Nawano, Masao;Yasuda, Kosuke;Takayama, Hiromitsu;
Journal Bioorganic & medicinal chemistry letters
Year 2020
DOI
S0960-894X(20)30354-1
URL
Keywords
type 2 diabetes hydrazone derivatives glucokinase activators herg inhibition

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