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.
Keywords:
Angiotensin II type 1 receptor antagonist; Antidiabetics; Antihypertensives; Drug discovery; Dual modulator; Fimasartan; PPARγ.
Copyright © 2018. Published by Elsevier Ltd.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiotensin II Type 1 Receptor Blockers / chemistry
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Angiotensin II Type 1 Receptor Blockers / pharmacokinetics
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Angiotensin II Type 1 Receptor Blockers / pharmacology*
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Animals
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Antihypertensive Agents / chemistry
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Antihypertensive Agents / pharmacokinetics
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Antihypertensive Agents / pharmacology
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Area Under Curve
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacokinetics
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Biphenyl Compounds / pharmacology*
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Disease Models, Animal
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Drug Discovery
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Drug Partial Agonism
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Half-Life
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / pharmacokinetics
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Hypoglycemic Agents / pharmacology
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PPAR gamma / agonists*
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Proof of Concept Study
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Pyrimidines / chemistry
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Pyrimidines / pharmacokinetics
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
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Tetrazoles / chemistry
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Tetrazoles / pharmacokinetics
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Tetrazoles / pharmacology*
Substances
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Angiotensin II Type 1 Receptor Blockers
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Antihypertensive Agents
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Biphenyl Compounds
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Hypoglycemic Agents
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PPAR gamma
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Pyrimidines
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Tetrazoles
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fimasartan