SYNTHESIS AND PRELIMINARY BIOLOGICAL EVALUATION OF 1-AMINOMETHYL-4-SUBSTITUTED-4H-PYRROLO[2,1-C][1,4] BENZOTHIAZINES, A NEW CLASS OF CALCIUM-ANTAGONISTS

被引:9
作者
CAMPIANI, G
NACCI, V
GAROFALO, A
BOTTA, M
FIORINI, I
TAFI, A
BRUNI, G
ROMEO, MR
PERES, A
BERTOLLINI, L
机构
[1] UNIV SIENA,DIPARTIMENTO FARM CHIM TECNOL,BANCHI SOTTO 55,I-53100 SIENA,ITALY
[2] UNIV SIENA,IST FARMACOL,I-53100 SIENA,ITALY
[3] UNIV MILANO,DIPARTIMENTO FISIOL & BIOCHIM GEN,I-20133 MILAN,ITALY
关键词
D O I
10.1016/S0960-894X(00)80212-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1193 / 1198
页数:6
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