Organic phosphorus compounds. IV. Asymmetric 4-(benzothiazol-2-yl)benzylphosphonates as potent calcium antagonistic vasodilators.
Various asymmetric or cyclic ester derivatives of the phosphonic acid moiety in the calcium antagonist fostedil (KB-944) were synthesized. The coronary vasodilator activity of these compounds was assessed by Langendorff's method. Among them, the ethyl isopropyl ester 12 showed the most potent activity, which was comparable to that of fostedil.
Yoshino
K
K
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
Goto
K
K
Kohno
T
T
Morita
T
T
Tsukamoto
G
G
D000818:Animals; D052160:Benzothiazoles; D002121:Calcium Channel Blockers / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D003326:Coronary Circulation / Q000187:drug effects; D004285:Dogs; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008297:Male; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D014665:Vasodilator Agents / Q000494:pharmacology*
D052160:Benzothiazoles; D002121:Calcium Channel Blockers; D009943:Organophosphorus Compounds; D013844:Thiazoles; D014665:Vasodilator Agents; C035950:fosfedil