SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF NEW 2-SUBSTITUTED 1,4-BENZOXAZINE DERIVATIVES

被引：0
作者：
KAJINO, M [1 ]
SHIBOUTA, Y [1 ]
NISHIKAWA, K [1 ]
MEGURO, K [1 ]
机构：
[1] TAKEDA CHEM IND LTD, DIV RES & DEV, BIOL RES LABS, OSAKA 532, JAPAN
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1991年 / 39卷 / 11期
关键词：
1,4-BENZOXAZINE; PIPERAZINE; CALMODULIN ANTAGONIST; ANTIHYPERTENSIVE ACTIVITY; INTRACELLULAR CALCIUM ANTAGONIST; SPONTANEOUSLY HYPERTENSIVE RAT;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of new 1,4-benzoxazine derivatives (XI, XII) possessing (4-phenyl-1-piperazinyl)alkyl moieties at the 2-position and related compounds (XIII) were synthesized and tested for calcium antagonistic, calmodulin antagonistic and antihypertensive activities. Various compounds had in vitro calmodulin antagonistic activity superior or comparable to that of trifluoperazine. Among these compounds, tetrahydronaphtho[2,3-b][1,4]oxazine derivatives such as 51, 53, 54, 58, 59, 60, 73 and 75 showed potent antihypertensive effects in spontaneously hypertensive rats. Optical isomers of 51 were also synthesized and evaluated biologically. No differences in biological activities were seen between the enantiomers.
引用
收藏
页码：2896 / 2905
页数：10
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