Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT1 and AT2 subtypes
Autor: | Ralph A. Rivero, Peter K. S. Siegl, K. L. Flanagan, Salah D. Kivlighn, Wallace T. Ashton, Gloria J. Zingaro, Tsing-Bau Chen, Victor J. Lotti, R. S. L. Chang, S. S. O'malley, W.J. Greenlee, Linda L. Chang |
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Rok vydání: | 1994 |
Předmět: |
endocrine system
Angiotensin receptor Angiotensin II receptor type 1 Stereochemistry Chemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Drug Discovery cardiovascular system Molecular Medicine Moiety Molecular Biology IC50 hormones hormone substitutes and hormone antagonists circulatory and respiratory physiology |
Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:2787-2792 |
ISSN: | 0960-894X |
DOI: | 10.1016/s0960-894x(01)80595-3 |
Popis: | A series of subnanomolar (IC50 triazolinone-based AT1/AT2-balanced AII antagonists has been identified. The 70-240-fold gain in AT2 activity relative to prototype compounds was achieved by the introduction of a 5-acylamino group on the N2-aryl moiety and the addition of (3-F-5'-Pr)biphenyl substituents on 4. These analogues exhibited AT2/AT1 IC50 rations of ≤1 in multiple assay systems including human adrenal. |
Databáze: | OpenAIRE |
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