The preparation of 4a-g, conformationally rigid calcium channel blockers related to Diltiazem, is described starting from tricyclic compounds 5a-c. On radioreceptor assay and preliminary biochemical tests some compounds show high affinity for Calcium Channel Receptors (CCRs) and calcium antagonistic activity comparable or superior to that of Diltiazem.
Synthesis and preliminary biological evaluation of 1-aminomethyl-4-substituted-4-H-pyrrolo[2,1-C][1,4] benzothiazines, a new class of calcium antagonists
PERES, ANTONIO;
1992-01-01
Abstract
The preparation of 4a-g, conformationally rigid calcium channel blockers related to Diltiazem, is described starting from tricyclic compounds 5a-c. On radioreceptor assay and preliminary biochemical tests some compounds show high affinity for Calcium Channel Receptors (CCRs) and calcium antagonistic activity comparable or superior to that of Diltiazem.
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