Syntheses and calcium channel antagonist activity of nifedipine analogues with methylsulfonylimidazolyl substituent.
Various diester analogues of nifedipine in which the ortho nitrophenyl group at position 4 is replaced by 1-methyl-2-methylsulfonyl-5-imidazolyl substituent, were synthesized and evaluated as calcium channel antagonists on guinea-pig ileal smooth muscle. Nifedipine was used as a standard. Compound 6n was found to be the most active.
Shafiee
A
A
Department of Chemistry, Faculty of Pharmacy, Medical Sciences University of Tehran, Iran.
Dehpour
A R
AR
Hadizadeh
F
F
Azimi
M
M
D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects / Q000378:metabolism; D009539:Nicotinic Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology
C114298:3-methyl-5-phenylethyl 1,4-dihydro-2,6-dimethyl-4-(1-methyl-2-methylsulfonyl-5-imidazolyl)-3,5-pyridinedicarboxylate; D002121:Calcium Channel Blockers; D009539:Nicotinic Acids; D009543:Nifedipine