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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological activity of novel substituted benzanilides as potassium channel activators. V.
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Synthesis and biological activity of novel substituted benzanilides as potassium channel activators. V.

机译：新型取代苯甲酰苯胺作为钾通道活化剂的合成及生物活性。 V.

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摘要

As part of our program toward designing potassium channel openers, the synthesis of a novel series of substituted benzanilides and their vasodilating activity are presented. The facile synthetic pathway generally involves coupling between the appropriate benzoyl chloride and commercial available anilines, followed by the selective or non-selective cleavage of methyl ether substituent(s), affording the corresponding phenol or bisphenol derivatives. The pharmacological evaluation of these structurally novel potential BK-openers on vascular contractile activity was studied in vitro, using isolated rat aortic rings pre-contracted with KCl 20 mM. Some derivatives were found to be potent smooth muscle relaxants and the vasodilation effects of these compounds were inhibited by tetraethylammonium (TEA) and iberiotoxin (IbTX), suggesting that the opening of BK channels is prevalent in the mechanism of action of these compounds. The best compound of the series was N-(2-hydroxy-5-phenyl)-(2-methoxy-5-chloro)-benzamide (16b) showing a full vasorelaxant efficacy and almost nanomolar potency index.
机译：作为设计钾通道开放剂的计划的一部分，我们提出了一系列新的取代苯甲酰苯胺的合成方法及其血管舒张活性。容易的合成途径通常包括合适的苯甲酰氯与市售苯胺之间的偶联，然后选择性或非选择性地裂解甲基醚取代基，得到相应的苯酚或双酚衍生物。在体外使用预先与KCl 20 mM缩合的离体大鼠主动脉环，研究了这些结构新颖的潜在BK-开启剂对血管收缩活性的药理学评价。已发现某些衍生物是有效的平滑肌松弛剂，并且四乙铵（TEA）和埃博毒素（IbTX）抑制了这些化合物的血管舒张作用，表明在这些化合物的作用机理中BK通道的开放是普遍的。该系列中最好的化合物是N-（2-羟基-5-苯基）-（2-甲氧基-5-氯）-苯甲酰胺（16b），具有完全的血管舒张功效，几乎具有纳摩尔效价指数。

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