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Synthesis and Calcium Antagonistic Activity of Some New 2‐Thioxo‐1,2,3,4‐tetrahydropyrimidine Derivatives
Author(s) -
Ertan Mevlüt,
Balkan Ayla,
Saraç Selma,
Uma Serdar,
Renaud Jean Francois,
Rollad Yves
Publication year - 1991
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19913240302
Subject(s) - thiourea , chemistry , ethanol , ethyl acetoacetate , potency , calcium , catalysis , microsome , stereochemistry , organic chemistry , in vitro , biochemistry
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 [ 3 H] PN 200—110 binding on microsomes obtained from rat skeletal muscle.