Acidic phenols: a new class of potent nonpeptide angiotensin II receptor antagonists

Autor:	W.J. Greenlee, Dorothy Levorse, Kenneth J. Fitch, Jim Tata, Peter K. S. Siegl, R. S. L. Chang, Karen Owens, Dooseop Kim, Tsing-Bau Chen, Gloria J. Zingaro, S. Scheck, Daljit S. Dhanoa, Nathan B. Mantlo, Salah D. Kivlighn
Rok vydání:	1994
Předmět:	Angiotensin receptor Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Biochemistry Angiotensin II chemistry.chemical_compound In vivo Drug Discovery Molecular Medicine Potency Phenols Receptor Molecular Biology IC50
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 4:207-212
ISSN:	0960-894X
Popis:	A series of imidazo[4,5-b]pyridine-based acidic phenols (Table 1,2) and biphenyl ethers (Table 3) are exemplified as novel non-peptide AII receptor antagonists. 0,0′-substituents which affect the acidity of the phenolic portion dramatically impact the activity of the compounds. The most potent antagonist in this series (Compound 13 , IC50 = 5 nM, rabbit aorta) exhibited good in vivo potency after both iv and oral administration to conscious rats.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::5b4edd3df3b4f383961e4375095d9fa8 https://doi.org/10.1016/s0960-894x(01)81148-3 Zobrazit plný text záznamu