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Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARĪ³ derived from the AT1R antagonist, Fimasartan.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Oct 15; Vol. 28 (19), pp. 3155-3160. Date of Electronic Publication: 2018 Aug 28. - Publication Year :
- 2018
-
Abstract
- Inspired by the well-known PPARĪ³ 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.<br /> (Copyright © 2018. Published by Elsevier Ltd.)
- Subjects :
- Angiotensin II Type 1 Receptor Blockers chemistry
Angiotensin II Type 1 Receptor Blockers pharmacokinetics
Animals
Antihypertensive Agents chemistry
Antihypertensive Agents pharmacokinetics
Antihypertensive Agents pharmacology
Area Under Curve
Biphenyl Compounds chemistry
Biphenyl Compounds pharmacokinetics
Disease Models, Animal
Drug Discovery
Drug Partial Agonism
Half-Life
Hypoglycemic Agents chemistry
Hypoglycemic Agents pharmacokinetics
Hypoglycemic Agents pharmacology
Proof of Concept Study
Pyrimidines chemistry
Pyrimidines pharmacokinetics
Structure-Activity Relationship
Tetrazoles chemistry
Tetrazoles pharmacokinetics
Angiotensin II Type 1 Receptor Blockers pharmacology
Biphenyl Compounds pharmacology
PPAR gamma agonists
Pyrimidines pharmacology
Tetrazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 28
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 30177375
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.08.036