2. Academic Validation
  3. Anti-adipogenic action of a novel oxazole derivative through activation of AMPK pathway

Anti-adipogenic action of a novel oxazole derivative through activation of AMPK pathway

  • Eur J Med Chem. 2023 Oct 20:262:115895. doi: 10.1016/j.ejmech.2023.115895.
Tripti Mishra 1,  Sanchita Gupta 2,  Prashant Rai 3,  Nilesh Khandelwal 2,  Mohit Chourasiya 4,  Vinita Kushwaha 2,  Astha Singh 2,  Salil Varshney 2,  Anil Nilkanth Gaikwad 5,  Tadigoppula Narender 6
Affiliations

Affiliations

  • 1 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India.
  • 2 Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
  • 3 Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India.
  • 4 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.
  • 5 Division of Pharmacology, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India. Electronic address: anil_gaikwad@cdri.res.in.
  • 6 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow, U.P., 226031, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India. Electronic address: t_narendra@cdri.res.in.
PMID: 37883898 DOI: 10.1016/j.ejmech.2023.115895
Abstract

Obesity is a chronic disorder with multifactorial etiology, including genetic, medical, dietary and Other environmental factors. Both natural and synthetic heterocyclic compounds, especially oxazoles, represent an interesting group of compounds and have gained much attention due to their remarkable biological activities. Therefore, a library of 3,3-DMAH (3,3-dimethylallylhalfordinol) inspired N-alkylated oxazole bromide salts with varied substitutions were prepared and screened using the 3T3-L1 model of adipogenesis and HFD-induced obesity model in Syrian golden hamsters. Several compounds in the synthesized series displayed remarkable anti-adipogenic potential on the differentiation of 3T3-L1 preadipocytes. Compound 19e, displayed the most potent activity of all and selected for further studies. Compound 19e inhibited mitotic clonal expansion of 3T3-L1 cells and enhanced the mitochondrial oxygen consumption rate of the cells during early phase of differentiation via AMPK activation. 19e also improved the dyslipidaemia in high calorie diet fed Syrian Golden Hamsters. Therefore, compound 19e can serve as a potential lead against adipogenesis and dyslipidaemia models and could be further investigated to affirm its significance as a drug candidate.

Keywords

3T3-L1 adipocytes; AMPK activation; Dyslipidaemia; Halfordinol; Oxazole derivatives; Oxygen consumption rate (OCR).

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