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Synthesis and evaluation of novel peptidomimetics bearing p-aminobenzoic acid moiety as potential antidiabetic agents.

Authors
  • Tang, Xue-Mei1, 2
  • Hu, Wen3
  • Fan, Li1
  • Wang, Hang1
  • Tang, Min-Hui1
  • Yang, Da-Cheng1
  • 1 Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry & Chemical Engineering, Institute of Bioorganic & Medicinal Chemistry, Southwest University, Chongqing, 400715, PR China. , (China)
  • 2 Key Laboratory of Freshwater Fish Reproduction & Development, Ministry of Education, Laboratory of Molecular Developmental Biology, School of Life Sciences, Southwest University, Chongqing, 400715, PR China. , (China)
  • 3 School of Chemistry & Chemical Engineering, Chongqing University, Chongqing, 400044, PR China. , (China)
Type
Published Article
Journal
Future Medicinal Chemistry
Publisher
"Future Science, LTD"
Publication Date
Jun 01, 2020
Volume
12
Issue
11
Pages
991–1013
Identifiers
DOI: 10.4155/fmc-2018-0372
PMID: 32208864
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

Aim: Search for a new class of potential antidiabetic agents. Methodology: A series of novel peptidomimetics bearing the p-aminobenzoic acid moiety (TM3-TM6) were designed and synthesized. For all synthetic target molecules, the peroxisome proliferator response element (PPRE) activated activities have been evaluated and the toxicity were computed. Results & discussion: 46 new p-aminobenzoic acid derivatives have been characterized by 1H NMR, 13C NMR and high-resolution mass spectrometry (HRMS). The results of in vitro PPRE-activated activity, molecular docking study and toxicity prediction revealed that these compounds had potential antidiabetic activities and low toxicity. In particular compound 3b had up to 87% PPRE-activated activity compared with pioglitazone. This discovery may provide new insights for finding novel PPRE lead compound.

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