Chromones。

Chemical immunology and allergy Pub Date : 2014-01-01 Epub Date: 2014-05-22 DOI:10.1159/000359986
Alan M Edwards
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引用次数: 0

摘要

色酮是一类化合物,其特征是在其化学组成中存在5:6苯-1:4吡酮结构。第一个临床使用的色素是khellin,它是从一种叫做Ammi visnaga的植物的种子中提取出来的,几个世纪以来,它一直被用作利尿剂和平滑肌松弛剂。1947年报道了它在支气管哮喘中的应用。20世纪50年代,本格实验室开始了一项研究计划,合成和开发用于治疗哮喘的克林的修饰物。通过动物模型和人体模型筛选新化合物,以检测化合物对致敏豚鼠肺组织胺和白三烯(SRS-A)过敏性释放的抑制作用,并检测其对吸入抗原支气管刺激引起的支气管收缩的抑制作用。最初的人体筛选工作由R.E.C. altonyan博士承担,他患有过敏性支气管哮喘,受雇于本格实验室。经过8年的时间,使用200多种化合物进行了600多次挑战,1965年,altonyan找到了cromoglyate二钠(DSCG),这种色素符合提供6小时以上保护的标准。DSCG至今仍被用作肥大细胞稳定剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Chromones.

The chromones are a class of chemical compounds characterised by the presence of the structure 5:6 benz-1:4-pyrone in their chemical make-up. The first chromone in clinical use, khellin, was extracted from the seeds of the plant Ammi visnaga, and had been used for centuries as a diuretic and as a smooth muscle relaxant. Its use in bronchial asthma was reported in 1947. In the 1950s, Benger's Laboratories embarked on a research programme to synthesise and develop modifications of khellin for the treatment of asthma. New compounds were screened using animal models to test the ability of the compound to prevent the anaphylactic release of histamine and SRS-A (leukotrienes) from sensitised guinea pig lung, and a human model to check the ability to reduce the bronchoconstriction induced by inhaled antigen bronchial challenge. For initial screening the human work was undertaken by Dr. R.E.C. Altounyan, who suffered from allergic bronchial asthma and was employed by Benger's Laboratories. After 8 years and more than 600 challenges using over 200 compounds, in 1965 Altounyan arrived at disodium cromoglycate (DSCG), the chromone that met the criteria of providing more than 6 h of protection. DSCG is still used today as a mast cell stabiliser.

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