几种水杨酸酯的合成及其生物活性

N. A. Bondareva, P. P. Purygin, Olga O. Isaeva
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引用次数: 0

摘要

水杨酸目前用途不大,但其衍生物是世界上最大的大吨位药物之一。然而,水杨酸的天然来源不能满足其制剂的需要,因此水杨酸及其衍生物只能通过人工合成的方法获得。水杨酸的衍生物由于其高反应性和在医疗实践中作为抗炎、解热、镇痛、抗菌、防腐和抗结核药物的广泛应用而引起了人们的极大兴趣。目前,关于水杨酸的各种衍生物的合成、结构和生物学性质的资料已经相当多,但需要注意的是,水杨酸的衍生物以及各种氨基酸和水杨酸的衍生物的研究还很少。研究水杨酸的新转化衍生物的性质具有广阔的前景,为实现这些新物质的结构固有的进一步化学修饰的潜力开辟了边界,这些化学修饰具有几个活性基团:羰基和羟基的组合。以水杨酸为基础的衍生物分子中的这种组合,其结构中含有已知的药理学基团,通常会导致新的高止血活性的出现。在我们的工作过程中,我们合成了一些基于水杨酸的酯类,并测定了第一个合成物质的抗血小板和抗凝血活性。对人捐献血液的体外凝血指标进行了研究。结果表明,所得化合物均具有抗聚集活性,其中部分化合物的抗聚集活性在10%以上。所有的实验工作是由我们的麻醉和重症监护的持续专业教育学院巴什基尔语国家卫生部医科大学的俄罗斯中央研究实验室的基础上巴什基尔语国家卫生部医科大学的俄罗斯和GBUZ岩石层命名的Kuvatova按照建议“指南的临床前研究新的药理物质。”
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Synthesis and biological activity of a number of salicylic acid esters
Salicylic acid is currently of little use, but its derivatives are one of the most large-tonnage drugs in the world. However, the natural sources of salicylic acid cannot satisfy the needs for its preparations and therefore the acid and its derivatives are obtained exclusively by synthetic means. Derivatives of salicylic acid are of great interest, due to their high reactivity and widespread use in medical practice as anti-inflammatory, antipyretic, analgesic, antimicrobial, antiseptic and anti-tuberculosis drugs. Currently, there is a fairly large body of data on the synthesis, structure, and biological properties of various derivatives of salicylic acid, however, it should be noted that derivatives of salicylic acid and various derivatives of amino acids and salicylic acid are poorly studied. The relevance of studying the properties of new transformed derivatives of salicylic acid is due to broad prospects that open the borders for realizing the potential for further chemical modification inherent in the structure of these new substances with a combination of several active groups: carbonyl and hydroxyl. Such a combination in a molecule of derivatives based on salicylic acid, containing known pharmacological groups in its structure, often leads to the appearance of a new high hemostatic activity. In the course of our work, we synthesized some esters based on salicylic acid, and also determined the antiplatelet and anticoagulant activity of the first synthesized substances. The study was conducted on the indicators of coagulogram in vitro on human donated blood. It was found that all provided compounds exhibit anti-aggregation activity, some of the compounds obtained by us exhibit anti-aggregation activity of more than 10%. All the experimental work was performed by us at the Department of Anesthesiology and Intensive Care with the course of the Institute of Continuing and Professional Education of the Bashkir State Medical University of the Ministry of Health of Russia on the basis of the Central Research Laboratory of the Bashkir State Medical University of the Ministry of Health of Russia and GBUZ RKB named after G.G. Kuvatova in accordance with the recommendations of the "Guidelines for the preclinical study of new pharmacological substances."
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