已批准的含炔药物：药代动力学性质及治疗应用综述

IF 5.9 2区医学 Q1 CHEMISTRY, MEDICINAL

European Journal of Medicinal Chemistry Pub Date : 2025-09-05 DOI:10.1016/j.ejmech.2025.118118

Jing Wang , Aiguo Gu , Huangdi Feng , Chuang Liu , Peng Li , Junhai Huang

{"title":"已批准的含炔药物：药代动力学性质及治疗应用综述","authors":"Jing Wang , Aiguo Gu , Huangdi Feng , Chuang Liu , Peng Li , Junhai Huang","doi":"10.1016/j.ejmech.2025.118118","DOIUrl":null,"url":null,"abstract":"<div><div>The alkynyl group is vital in organic chemistry. It frequently occurs in natural compounds. Alkynyl -containing pharmaceuticals include contraceptive, anti-Parkinsonian, anti-HIV, and antifungal agents. Incorporating the alkynyl group improves physicochemical properties by enhancing metabolic stability, optimizing pharmacokinetics, and increasing targeting selectivity. Consequently, alkynyl-containing drugs show favorable pharmacological and pharmacokinetic profiles, prompting medicinal chemists to develop many such drugs, several of which have been approved commercially. This review summarizes the effects, mechanisms, and pharmacokinetics of Alkynyl-containing drugs approved between 1960 and 2025.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"300 ","pages":"Article 118118"},"PeriodicalIF":5.9000,"publicationDate":"2025-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Approved alkyne-containing drugs: A review of their pharmacokinetic properties and therapeutic applications\",\"authors\":\"Jing Wang , Aiguo Gu , Huangdi Feng , Chuang Liu , Peng Li , Junhai Huang\",\"doi\":\"10.1016/j.ejmech.2025.118118\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>The alkynyl group is vital in organic chemistry. It frequently occurs in natural compounds. Alkynyl -containing pharmaceuticals include contraceptive, anti-Parkinsonian, anti-HIV, and antifungal agents. Incorporating the alkynyl group improves physicochemical properties by enhancing metabolic stability, optimizing pharmacokinetics, and increasing targeting selectivity. Consequently, alkynyl-containing drugs show favorable pharmacological and pharmacokinetic profiles, prompting medicinal chemists to develop many such drugs, several of which have been approved commercially. This review summarizes the effects, mechanisms, and pharmacokinetics of Alkynyl-containing drugs approved between 1960 and 2025.</div></div>\",\"PeriodicalId\":314,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry\",\"volume\":\"300 \",\"pages\":\"Article 118118\"},\"PeriodicalIF\":5.9000,\"publicationDate\":\"2025-09-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0223523425008839\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0223523425008839","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}

引用次数: 0

摘要

炔基在有机化学中是很重要的。它经常出现在天然化合物中。含炔基的药物包括避孕药、抗帕金森病、抗hiv和抗真菌药物。加入炔基通过增强代谢稳定性、优化药代动力学和增加靶向选择性来改善理化性质。因此，含炔基的药物表现出良好的药理学和药代动力学特征，促使药物化学家开发出许多此类药物，其中一些已获得商业批准。本文综述了1960年至2025年间批准的含炔基药物的作用、机制和药代动力学。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Approved alkyne-containing drugs: A review of their pharmacokinetic properties and therapeutic applications

查看原文本刊更多论文

Approved alkyne-containing drugs: A review of their pharmacokinetic properties and therapeutic applications

The alkynyl group is vital in organic chemistry. It frequently occurs in natural compounds. Alkynyl -containing pharmaceuticals include contraceptive, anti-Parkinsonian, anti-HIV, and antifungal agents. Incorporating the alkynyl group improves physicochemical properties by enhancing metabolic stability, optimizing pharmacokinetics, and increasing targeting selectivity. Consequently, alkynyl-containing drugs show favorable pharmacological and pharmacokinetic profiles, prompting medicinal chemists to develop many such drugs, several of which have been approved commercially. This review summarizes the effects, mechanisms, and pharmacokinetics of Alkynyl-containing drugs approved between 1960 and 2025.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

European Journal of Medicinal Chemistry 化学-医药化学

CiteScore

11.70

自引率

9.00%

发文量

863

审稿时长

29 days

期刊介绍： The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.