QUINAZOLINONE BIPHENYL ACYLSULFONAMIDES - A POTENT NEW CLASS OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS

Authors
CHAKRAVARTY PK STRELITZ RA CHEN TB CHANG RSL LOTTI VJ ZINGARO GJ SCHORN TW KIVLIGHN SD SIEGL PKS PATCHETT AA GREENLEE WJ
Citation
Pk. Chakravarty et al., QUINAZOLINONE BIPHENYL ACYLSULFONAMIDES - A POTENT NEW CLASS OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 4(1), 1994, pp. 75-80
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
1
Year of publication
1994
Pages
75 - 80
Database
ISI
SICI code
0960-894X(1994)4:1<75:QBA-AP>2.0.ZU;2-5
Abstract
A new series of quinazolinone-based AT(1) selective antagonists, beari ng acylsulfonamides (-SO(2)NHCOR) as the tetrazole bioisosteres, was e valuated. While AT(1) potencies remained similar to the tetrazole anal ogs, the AT(2) receptor affinities were significantly improved with th e introduction of acylsulfonamide groups. Several of these antagonists displayed improved in vivo properties.