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一系列呋喃[3,2-b]吲哚类化合物对人类嗜碱性白细胞组胺释放具有抑制作用,随后,对其在化学结构上进行了修饰,制备了一系列吲哚酰胺基四唑类化合物。其中CI-949(5-甲氧基-3-(1-甲基乙氧基)-1-苯基-N-1H-四唑-5-基-1H-吲哚-2-羧酰胺精氨酸盐)为临床上有希望的抗过敏药。结构-活性关系的研究通过检测酰胺基四唑类对由抗-IgE抗体引起的人类白细胞组胺释放有无抑制作用,研究其结构与活性的关系。凡吲哚核上含有3-烷氧基、5-甲氧基以及1-苯基取代基的化合物都具有令人满意的抑制组胺释放作用(表1,略)。药物活性有赖于吲哚5位或6位(R_1)上甲氧基或卤素的取代,在吲哚1位(R_2)上由苯基取代,其活性大于用烷基取
A series of furan [3,2-b] indoles inhibit the release of histamine from human basophils, and subsequently their chemical structure has been modified to prepare a series of indole amide tetrazoles Compound. Wherein CI-949 (5-methoxy-3- (1-methylethoxy) -1-phenyl-N-1H-tetrazol-5-yl-1H-indole-2-carboxamide arginine Acid salt) is a clinically promising anti-allergy drug. Structure-activity relationship Study on the structure and activity of amidotetrazoles by anti-IgE antibody-induced human leukocyte histamine release inhibition. All indole nuclei containing 3-alkoxy, 5-methoxy and 1-phenyl substituents have satisfactory histamine release inhibitory effect (Table 1, omitted). The drug activity depends on the substitution of methoxy or halogen on the 5-position or 6-position (R_1) of indole, which is substituted by phenyl on the 1-position of indole (R_2)