DHPM-thiones及其衍生物的结构和功能方面:对制药潜力的批判性审查
Artyom Savelyev1, Dmitriy Khrustalev1, Irina Losseva1
1School of Pharmacy, NPJSC "Karaganda Medical University", 40 Gogol St., Karaganda 100008, Kazakhstan.
二皮里米丁 (DHPs) 显示出对抗耐药性和病毒感染的新药的前景. 最近的研究突出了合成的进步和强大的临床前结果,表明未来的临床试验.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药物发现 药物发现 药物发现
背景情况:
- 二皮里米丁 (DHP) 和它们的类衍生物是新药开发的关键支架.
- 解决抗微生物耐药性和COVID后治疗缺口等挑战需要创新的制药解决方案.
- DHPs为开发新的治疗药物提供了一个多功能平台.
研究的目的:
- 系统地审查最近 (2020-2025) 在二皮里米丁合成和应用中的进展.
- 评估DHP衍生物的结构-活性关系 (SAR) 和临床前潜力.
- 确定基于DHP的药物发现的新兴趋势和未来方向.
主要方法:
- 系统的文献审查遵循PRISMA指南.
- 包括Scopus,PubMed和Web of Science在内的电子数据库的全面搜索.
- 来自60项选定的原始研究 (2020-2025) 数据的定性综合.
主要成果:
- 自2020年以来,DHP研究出版物的显著增加.
- 关键的结构修改,如N-甲基化和C4/C5替代,提高生物利用性和效力.
- 对病毒蛋白酶和各种癌症细胞系表现出强大的抑制活性.
结论:
- DHP架构在药物开发方面具有显著的翻译潜力.
- 像LaSOM 65和Ru (II) -Biginelli杂交物等值得注意的化合物显示出有希望的结果.
- 该领域已准备好进行推进,到2030年有可能进行第一阶段试验.
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