Synthesis, chemical and pharmacological properties of some 4-aryl-1,2,3,4,5,6,7,8-octahydroquinazoline-2,5-diones.
A series of 4-aryl-1,2,3,4,5,6,7,8-octahydroquinazoline-2,5-diones were synthesized by condensing urea with 1,3-cyclohexanedione and appropriate aromatic aldehydes according to the Biginelli reaction. The structures of the compounds were confirmed by elementary and spectroscopic analysis. The compounds synthesized were tested in vitro for their calcium antagonistic activities. BaCl2-induced contractions of rat ileum were inhibited dose-dependently. Compounds 3-8 exerted weak calcium antagonistic activity on smooth muscles compared with the standard nicardipine.
Saraç
S
S
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.
Yarim
M
M
Ertan
M
M
Boydağ
S
S
Erol
K
K
D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D009126:Muscle Relaxation / Q000187:drug effects; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
D002121:Calcium Channel Blockers; D011799:Quinazolines