Synthesis and evaluation of novel peptidomimetics bearing p-aminobenzoic acid moiety as potential antidiabetic agents.
Future Med Chem
; 12(11): 991-1013, 2020 06.
Article
in En
| MEDLINE
| ID: mdl-32208864
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.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
4-Aminobenzoic Acid
/
PPAR gamma
/
Diabetes Mellitus
/
Peptidomimetics
/
Hypoglycemic Agents
Type of study:
Prognostic_studies
Limits:
Humans
Language:
En
Journal:
Future Med Chem
Year:
2020
Document type:
Article