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Peer-reviewed veterinary case report

Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2018
Authors:
Choung, Wonken et al.
Affiliation:
Research Center · South Korea

Abstract

Inspired by the well-known PPARγ partial agonism of angiotensin II type 1 receptor (AT1R) antagonists exemplified by an antihypertensive drug, Telmisartan, efforts to identify compounds with the dual activities have been pursued in order to control the two major metabolic disorders, hypertension and hyperglycemia simultaneously. Lead compound 18 derived from the AT1R antagonist, Fimasartan, has successfully presented the possibility to control the medical conditions by a single molecule.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/30177375/