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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Inhibition of alpha-glucosidase and alpha-amylase by diaryl derivatives of imidazole-thione and 1,2,4-triazole-thiol.
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Inhibition of alpha-glucosidase and alpha-amylase by diaryl derivatives of imidazole-thione and 1,2,4-triazole-thiol.

机译：咪唑-硫酮和1,2,4-三唑-硫醇的二芳基衍生物对α-葡萄糖苷酶和α-淀粉酶的抑制作用。

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摘要

The in vivo and in vitro effects of 4,5-diphenylimidazole-2-thione (1), 4,5-diphenyl-1,2,4-triazole-3-thiol (2) and 5-(2-hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thiol (3) on alpha-glucosidase and alpha-amylase were investigated. The in vivo inhibition has been found to be dose-dependent and to occur at a value less than LD50. The in vitro treatment of the enzymes by 4,5-diphenylimidazole-2-thione exhibited a reversible inhibition of the non-competitive type with Ki value of 3.5 and 6.5x10(-5) M for alpha-glucosidase and alpha-amylase, respectively. 4,5-diphenyl-1,2,4-triazole-3-thione showed a reversible inhibition of the competitive and non-competitive types, with Ki value of 10(-5) M magnitude, for alpha-glucosidase and alpha-amylase. On the other hand, 5-(o-hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thione did not display an inhibitory effect towards alpha-amylase but showed a potent inhibition of the competitive type for hepatic alpha-glucosidase with 10(-5) M magnitude of Ki value.
机译：4,5-二苯基咪唑-2-硫酮（1），4,5-二苯基-1,2,4-三唑-3-硫醇（2）和5-（2-羟苯基）-的体内和体外作用研究了α-葡萄糖苷酶和α-淀粉酶上的4-苯基-1,2,4-三唑-3-硫醇（3）。已经发现体内抑制是剂量依赖性的并且以小于LD 50的值发生。 4,5-二苯基咪唑-2-硫酮对酶的体外处理显示出非竞争性类型的可逆抑制，α-葡萄糖苷酶和α-淀粉酶的Ki值分别为3.5和6.5x10（-5）M 。 4,5-二苯基-1,2,4-三唑-3-硫酮对α-葡萄糖苷酶和α-淀粉酶显示出可逆性抑制竞争型和非竞争型，Ki值为10（-5）M量级。另一方面，5-（邻-羟基苯基）-4-苯基-1,2,4-三唑-3-硫酮对α-淀粉酶没有抑制作用，但对肝α-竞争型表现出有效的抑制作用。 -葡糖苷酶的Ki值为10（-5）M。

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