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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors
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Trimethoprim and other nonclassical antifolates an excellent template for searching modifications of dihydrofolate reductase enzyme inhibitors

机译：Trimethokim和其他非化学防雾的优异模板，用于搜索二氢脱水还原酶酶抑制剂的改性

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摘要

The development of new mechanisms of resistance among pathogens, the occurrence and transmission of genes responsible for antibiotic insensitivity, as well as cancer diseases have been a serious clinical problem around the world for over 50 years. Therefore, intense searching of new leading structures and active substances, which may be used as new drugs, especially against strain resistant to all available therapeutics, is very important. Dihydrofolate reductase (DHFR) has attracted a lot of attention as a molecular target for bacterial resistance over several decades, resulting in a number of useful agents. Trimethoprim (TMP), (2,4-diamino-5-(3 ',4 ',5 '-trimethoxybenzyl)pyrimidine) is the well-known dihydrofolate reductase inhibitor and one of the standard antibiotics used in urinary tract infections (UTIs). This review highlights advances in design, synthesis, and biological evaluations in structural modifications of TMP as DHFR inhibitors. In addition, this report presents the differences in the active site of human and pathogen DHFR. Moreover, an excellent review of DHFR inhibition and their relevance to antimicrobial and parasitic chemotherapy was presented.
机译：在病原体中抗性的新机制，对抗生素不敏感的基因的发生和传播，以及癌症疾病在世界各地是一个超过50年的严重临床问题。因此，对新的领先结构和活性物质的激烈寻求可以用作新药物，特别是对所有可用治疗的应变，非常重要。二氢氟乙酯还原酶（DHFR）吸引了大量关注，作为几十年的细菌耐药的分子靶标，导致许多有用的药剂。 Trimethokim（TMP），（2,4-二氨基-5-（3'，4'，5'-三甲氧基苄基）嘧啶是众所周知的二氢醇还原酶抑制剂和尿路感染中使用的标准抗生素之一（UTI） 。本综述突出显示了TMP作为DHFR抑制剂的结构修饰中的设计，合成和生物学评价的进步。此外，本报告提出了人和病原体DHFR活性位点的差异。此外，介绍了对DHFR抑制的出色综述及其与抗菌和寄生化疗的相关性。

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