Synthesis and calcium antagonistic activity of some new 2-thioxo-1,2,3,4-tetrahydropyrimidine derivatives.
A series of 1,2,3,4-tetrahydro-6-methyl-4-(substituted phenyl)-2-thioxo-5-pyrimidinecarboxylic acid methyl esters were synthesized by condensing thiourea with methyl acetoacetate and nonsubstituted or differently substituted benzaldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures of the compounds were confirmed by elemental and spectroscopic analysis. -The compounds were evaluated for their calcium antagonistic activity on the basis of their potency in inhibiting [3H] PN 200-110 binding on microsomes obtained from rat skeletal muscle.
Ertan
M
M
Hacettepe University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
Balkan
A
A
Saraç
S
S
Uma
S
S
Renaud
J F
JF
Rollad
Y
Y
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D017275:Isradipine; D008861:Microsomes / Q000187:drug effects / Q000378:metabolism; D010069:Oxadiazoles / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013871:Thiones / Q000138:chemical synthesis / Q000494:pharmacology
D002121:Calcium Channel Blockers; D010069:Oxadiazoles; D011743:Pyrimidines; D013871:Thiones; D017275:Isradipine