Synthesis and calcium antagonistic activity of some new 2-thioxo-1,2,3,4-tetrahydropyrimidine derivatives

Arch Pharm (Weinheim). 1991 Mar;324(3):135-9. doi: 10.1002/ardp.19913240302.

Abstract

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.

MeSH terms

  • Animals
  • Binding, Competitive / drug effects
  • Calcium Channel Blockers / chemical synthesis*
  • Calcium Channel Blockers / pharmacology
  • In Vitro Techniques
  • Isradipine
  • Microsomes / drug effects
  • Microsomes / metabolism
  • Oxadiazoles / metabolism
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Rats
  • Thiones / chemical synthesis
  • Thiones / pharmacology

Substances

  • Calcium Channel Blockers
  • Oxadiazoles
  • Pyrimidines
  • Thiones
  • Isradipine