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

Search for a new class of potential antidiabetic agents. A series of novel peptidomimetics bearing the -aminobenzoic acid moiety ( - ) were designed and synthesized. For all synthetic target molecules, the peroxisome proliferator response element (PPRE) activated activities have been evaluated and t...

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Bibliographic Details
Published in:Future medicinal chemistry 2020-06, Vol.12 (11), p.991-1013
Main Authors: Tang, Xue-Mei, Hu, Wen, Fan, Li, Wang, Hang, Tang, Min-Hui, Yang, Da-Cheng
Format: Article
Language:English
Subjects:
4-Aminobenzoic Acid - chemistry
4-Aminobenzoic Acid - pharmacology
Amino acids
Antidiabetics
Cardiovascular disease
Chromatography
Diabetes
Diabetes mellitus
Diabetes Mellitus - drug therapy
Diabetes Mellitus - metabolism
Drugs
Gene expression
Humans
Hypoglycemic Agents - chemical synthesis
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacology
Insulin resistance
Mass spectroscopy
Metabolism
Molecular Docking Simulation
Molecular Structure
NMR
Nuclear magnetic resonance
para-Aminobenzoic acid
Peptides
Peptidomimetics
Peptidomimetics - chemical synthesis
Peptidomimetics - chemistry
Peptidomimetics - pharmacology
Pioglitazone
PPAR gamma - antagonists & inhibitors
PPAR gamma - metabolism
Toxicity
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Summary:Search for a new class of potential antidiabetic agents. A series of novel peptidomimetics bearing the -aminobenzoic acid moiety ( - ) 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. 46 new -aminobenzoic acid derivatives have been characterized by H NMR, C NMR and high-resolution mass spectrometry (HRMS). The results of PPRE-activated activity, molecular docking study and toxicity prediction revealed that these compounds had potential antidiabetic activities and low toxicity. In particular compound had up to 87% PPRE-activated activity compared with pioglitazone. This discovery may provide new insights for finding novel PPRE lead compound.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2018-0372