Synthesis and preliminary biological evaluation of 4,6-disubstituted 3-cyanopyridin-2(1H)-ones, a new class of calcium entry blockers.
The preparation of 3-cyano-4,6-diaryl-pyridin-2(1H)-ones 4a-h, calcium entry blockers related to diltiazem, is described starting from 1,3-diaryl-2-propen-1-ones 5. On preliminary pharmacological tests all compounds are active and some of them show calcium antagonistic activity superior or comparable to diltiazem.
Manna
F
F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamcnte Attive, Università di Roma La Sapienza, Rome, Italy. fmanna@uniromal.it
Chimenti
F
F
Bolasco
A
A
Bizzarri
B
B
Botta
M
M
Tafi
A
A
Filippelli
A
A
Rossi
S
S
D000818:Animals; D001011:Aorta / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004110:Diltiazem / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D066298:In Vitro Techniques; D008956:Models, Chemical; D015394:Molecular Structure; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D011728:Pyridones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats
D002121:Calcium Channel Blockers; D011728:Pyridones; D004110:Diltiazem