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自发现异烟肼近三十年来,新的抗结核药物出现的不多。目前第一线抗结核药仍为链霉素、异烟肼和对氨基水杨酸(以下称 PAS)。但是,寻找新的抗结核药物的研究工作始终在进行着。这方面工作包括:对原有药物进行一系列结构改造,试图得到活性更高,尤其对耐药结核菌更敏感、副作用更低的衍生物;同时亦积极筛选新型抗结核药物。下面将这方面研究情况作一简单介绍。对氨基水杨酸及其衍生物目前,PAS 仍为抗结核的首选药物之一。其缺点是刺激性较大,排泄较快。若制成对氨基水杨酸钙铝盐、苯甲酰胺水杨酸钙、对氨基水杨酸苯酯等衍生物后,可延长作用时间或减缓对消化道的刺激。有人亦将 PAS 作成肌醇酯。如:Hexakis-o-(p-aminosali-cylyl)-muco-inositol(Ⅰ)(本文的化学结构式均见附图)。
Nearly 30 years since the discovery of isoniazid, the new anti-TB drugs appear not much. Currently the first-line anti-TB drugs are still streptomycin, isoniazid and p-aminosalicylic acid (hereinafter referred to as PAS). However, the search for new anti-tuberculosis drugs is still ongoing. Work in this area includes: a series of structural reorganizations of existing drugs in an attempt to obtain more active compounds, especially those that are more sensitive to drug-resistant TB and have fewer side effects; and actively screening new types of anti-tuberculosis drugs. The following research situation in this area for a brief introduction. Aspirin and its derivatives Currently, PAS is still one of the preferred anti-TB drugs. The disadvantage is irritation, excretion faster. If made of calcium aluminum amino acid salicylate, benzamide calcium salicylate, p-amino phenyl salicylate and other derivatives, can extend the action time or slow down the stimulation of the digestive tract. Someone also make inositol esters of PAS. Such as: Hexakis-o- (p-aminosali-cylyl) -muco-inositol (Ⅰ) (the chemical structure of this article are shown in the accompanying drawings).