Synthesis of angiotensin II antagonists with variations in position 5.
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.
Nyéki
O
O
Chemical Works of Gedeon Richter, Ltd., Budapest, Hungary.
Szalay
K S
KS
Kisfaludy
L
L
Kárpáti
E
E
Szporny
L
L
Makara
G B
GB
Varga
B
B
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
D000804:Angiotensin II