NO-independent stimulators of soluble guanylate cyclase.
SARs around a novel type of guanylate cyclase stimulator which act by a mechanism different from classical NO-donors are described. Several pyrazolopyridinylpyrimidines are shown to relax aortic rings and revealed a long-lasting blood pressure lowering effect in rats after oral application.
Institute of Medicinal Chemistry, Pharma Research Centre, Bayer AG, Wuppertal, FRG. alexander.straub.as@bayer-ag.de
A
A
Straub
J P
JP
Stasch
C
C
Alonso-Alija
J
J
Benet-Buchholz
B
B
Ducke
A
A
Feurer
C
C
Fürstner
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D020536:Enzyme Activators / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006162:Guanylate Cyclase / Q000378:metabolism*; D007191:Indazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits; D013329:Structure-Activity Relationship; D014664:Vasodilation / Q000187:drug effects
C423582:3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo(3,4-b)pyridine; D020536:Enzyme Activators; D007191:Indazoles; D011720:Pyrazoles; D011725:Pyridines; C090937:3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole; D006162:Guanylate Cyclase