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Design, synthesis, and pharmacological evaluation of 2-(4-sulfonylphenyl)-2-[(E)-pyrrolidin-1-ylimino]-N-thiazoleacetamides as glucokinase activators.
- 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.)
- Subjects :
- Acetamides administration & dosage
Acetamides chemical synthesis
Administration, Oral
Animals
Blood Glucose drug effects
Diabetes Mellitus, Experimental metabolism
Diabetes Mellitus, Type 2 metabolism
Dose-Response Relationship, Drug
Drug Design
Glucokinase metabolism
Hypoglycemic Agents administration & dosage
Hypoglycemic Agents chemical synthesis
Mice
Mice, Inbred C57BL
Molecular Structure
Rats
Rats, Sprague-Dawley
Structure-Activity Relationship
Thiazoles administration & dosage
Thiazoles chemical synthesis
Acetamides pharmacology
Diabetes Mellitus, Experimental drug therapy
Diabetes Mellitus, Type 2 drug therapy
Glucokinase antagonists & inhibitors
Hypoglycemic Agents pharmacology
Thiazoles pharmacology
Subjects
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