Structure-activity relationship studies in the field of calcium antagonists. Xanthone 1,4-dihydropyridines bearing a 2,3-lactone ring.
A series of xanthone 1,4-dihydropyridine derivatives bearing a 2,3-lactone ring and a 2-acetoxymethyl group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonist properties. The introduction of a 2,3-lactone ring improved the negative inotropic activity and selectivity.
D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D007783:Lactones / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D009200:Myocardial Contraction / Q000187:drug effects; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers; D007783:Lactones; D011725:Pyridines; C014047:hydroxypyridines