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鉴于拟交感胺分子结构的特点和溴苄乙铵构效关系的研究,用苯的同电异素体噻吩等代替,设计合成噻吩季铵盐衍生物(1)。因溴苄乙胺属季铵盐化合物,故胃肠道吸收不规则。胍乙啶是一有效的降压药,无季铵盐吸收不规则的缺点。又据报道,苯甲胍及其邻位卤代物,不同于胍乙啶系通过阻滞去甲肾上腺素的储存而降压,而是通过抑制去甲肾上腺素的释放,导
In view of the characteristics of the structure of the sympathetic amines and the structure-activity relationship of benzylbenzyl, the thiophene quaternary ammonium salt derivatives (1) were designed and synthesized by replacing the benzene isolethiophene thiophene and the like. Bromobenzene ethylamine is a quaternary ammonium compound, so the gastrointestinal absorption irregular. Guanethidine is an effective antihypertensive drug without the drawback of irregular absorption of quaternary ammonium salts. It has also been reported that benzoguanidine and its vicinal halogens, unlike guanethidine, depressurization by blocking the storage of norepinephrine but rather by inhibiting the release of norepinephrine