Structure-activity relationship studies of xanthone and fluorenone-1,4-dihydropyridine-5-phosphonates.
A series of xanthone and fluorenone-1,4-dihydropyridine derivatives bearing a 5-phosphonate group were prepared. The compounds were evaluated for inotropic, chronotropic and calcium antagonistic properties. The insertion of a phosphonate group is detrimental for inotropic and calcium antagonistic activity but improves the potency and selectivity for chronotropism.
Budriesi
R
R
Department of Pharmaceutical Sciences, University of Bologna, Italy.
Rampa
A
A
Bisi
A
A
Fabbri
G
G
Chiarini
A
A
Valenti
P
P
D000818:Animals; D001013:Aorta, Thoracic / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004095:Dihydropyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D066298:In Vitro Techniques; 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; D009943:Organophosphorus Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D002121:Calcium Channel Blockers; D002316:Cardiotonic Agents; D004095:Dihydropyridines; D009943:Organophosphorus Compounds