Synthesis and adrenergic .BETA.-blocking activity of some propanolamine derivatives.
作者:HIROYUKI OBASE、HIDEKO TATSUNO、KATSUTOSHI GOTO、KOKI SHIGENOBU、YUTAKA KASUYA、YOSHIYUKI YAMADA、KYOICHI FUJII、SEIICHI YADA
DOI:10.1248/cpb.26.1443
日期:——
Some propanolamine derivatives were synthesized and their β-adrenergic blocking activities were determined. Among the compounds tested, all compounds with benzothiazole nucleus were found to have potent β-adrenergic blocking activity, and those with other nuclei failed to produce substantial β-blocking activity with one exception. Three compounds with benzothiazole nucleus were more potent than sotalol in their β-blocking activity, and the other two were equipotent to sotalol. One with benzotriazole nucleus had about the same β-blocking activity as sotalol.
合成了一些丙醇胺衍生物,并确定了它们的β-肾上腺素能阻滞活性。在测试的化合物中,所有含有苯并噻唑核的化合物均显示出强的β-肾上腺素能阻滞活性,而其他核的化合物则未能产生实质性的β-阻滞活性,只有一个例外。三种含有苯并噻唑核的化合物在β-阻滞活性方面比索他洛尔更强,其他两种与索他洛尔的效力相当。一个含有苯并三氮杂核的化合物的β-阻滞活性与索他洛尔大致相同。