title: Synthesis of angiotensin II antagonists with variations in position 5.
abstract: Six angiotensin II antagonists containing cyclohexylglycine (Chg) or cyclopentylglycine (Cpg) in position 5 were synthesized by stepwise elongation in solution, using the pentafluorophenyl ester method. The influence of substitution on the inhibitory properties of the analogues was studied in four different bioassays. [Sar1,Chg5,Lac8]AII proved to be the most potent antagonist with low intrinsic activity in both the in vitro and in vivo tests.
authors: Chemical Works of Gedeon Richter, Ltd., Budapest, Hungary.
authors: O
authors: O
authors: Nyéki
authors: K S
authors: KS
authors: Szalay
authors: L
authors: L
authors: Kisfaludy
authors: E
authors: E
authors: Kárpáti
authors: L
authors: L
authors: Szporny
authors: G B
authors: GB
authors: Makara
authors: B
authors: B
authors: Varga
mesh_terms: D000804:Angiotensin II / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors*; D000818:Animals; D001681:Biological Assay; D001794:Blood Pressure / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000804:Angiotensin II