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本文摘自一期由24篇文章组成的特辑,叙述一种新型的呼吸道疾病治疗剂noleptan的有关化学、药理学、生物化学、畸胎学以及临床研究等各方面的问题。结果提示,这一新药具有:①可提高病理性的血氧分压;②刺激呼吸作用;③镇咳作用等三方面的效应,符合治疗呼吸道疾病的要求。化学研究:在取代苄胺衍生物中,bisolvon(Ⅰ)是一种治疗支气管疾患的有效药物。进一步研究一系列N-苄基取代氨基烷酸及其衍生物(Ⅱ)时发现,大多数化合物毒性较小,具有镇咳作用,并有刺激呼吸作用,其中化合物Ⅲ(Forminoben·HCl,PB-89,Noleptan)的作用最为显著。合成方法如下:2-苯甲酰氨-6-氯甲苯(0.68克分子)悬浮于四氯化碳(4.5升)中,在紫外线照射及回流
This article is an extract from a 24-issue monograph that addresses a variety of issues related to chemistry, pharmacology, biochemistry, teratology and clinical research of a novel noleptan for the treatment of respiratory diseases. The results suggest that this new drug has: ① can increase the pathological partial pressure of oxygen; ② stimulate respiration; ③ antitussive effect of three aspects of the effect, in line with the requirements of the treatment of respiratory diseases. Chemical Research: Among the substituted benzylamine derivatives, bisolvon (I) is a potent drug for the treatment of bronchial disorders. Further investigation of a series of N-benzyl substituted aminoalkanoic acids and their derivatives (II) showed that most of the compounds were less toxic, had antitussive action and had respiratory stimulatory effects. Among them, Compound Ⅲ (Forminoben · HCl, PB- 89, Noleptan) the most significant role. The synthesis was as follows: 2-Benzoylamino-6-chlorotoluene (0.68 mol) was suspended in carbon tetrachloride (4.5 L) and irradiated with UV light and reflux