title: Novel paramagnetic AT1 receptor antagonists.
abstract: Novel paramagnetic selective angiotensin AT(1) receptor antagonists (sartans) bearing nitroxides (3, 4) have been prepared and their pharmacology evaluated in vitro as well as in vivo. Compounds 3, 4 proved to be effective sartans with pK(B) estimates in the range 6.2-9.1. In addition, the sodium salt (11) of 4 (R = Bu) is able to protect against vascular injury in hypertensive rats as determined by its ability to attenuate the development of intimal thickening caused by balloon injury of the carotid artery.
authors.affiliation: ARC Centre of Excellence for Free Radical Chemistry and Biotechnology, Victoria, Australia.
authors.forename: Nichole P H
authors.initials: NP
authors.lastname: Tan
authors.forename: Michelle K
authors.initials: MK
authors.lastname: Taylor
authors.forename: Steven E
authors.initials: SE
authors.lastname: Bottle
authors.forename: Christine E
authors.initials: CE
authors.lastname: Wright
authors.forename: James
authors.initials: J
authors.lastname: Ziogas
authors.forename: Jonathan M
authors.initials: JM
authors.lastname: White
authors.forename: Carl H
authors.initials: CH
authors.lastname: Schiesser
authors.forename: Nitya V
authors.initials: NV
authors.lastname: Jani
mesh_terms: D047228:Angiotensin II Type 1 Receptor Blockers / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D001011:Aorta / Q000187:drug effects / Q000378:metabolism; D001794:Blood Pressure / Q000187:drug effects; D016466:CHO Cells; D002339:Carotid Arteries / Q000187:drug effects / Q000473:pathology; D002404:Catheterization; D006224:Cricetinae; D003412:Cricetulus; D006973:Hypertension / Q000188:drug therapy* / Q000473:pathology / Q000503:physiopathology; D066298:In Vitro Techniques; D060328:Magnetic Phenomena; D008297:Male; D009249:NADP / Q000494:pharmacology; D009589:Nitrogen Oxides / Q000737:chemistry*; D051381:Rats; D011918:Rats, Inbred SHR; D013481:Superoxides / Q000378:metabolism; D017539:Tunica Intima / Q000187:drug effects / Q000293:injuries / Q000473:pathology
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D009589:Nitrogen Oxides; D013481:Superoxides; D009249:NADP; C039900:nitroxyl