New 1,2,3-triazole-linked (±)-agrimonolide derivatives as anti-ulcerative colitis agents inhibiting JAK1/STAT3 pathways.

IF 3.8 2区化学 Q2 CHEMISTRY, APPLIED

Molecular Diversity Pub Date : 2025-09-23 DOI:10.1007/s11030-025-11368-3

Xiao Zhang, Ming-Qian Ju, Heng-Li Yang, Chun-Fei Zhang, Mao-Kui Huang, Yan-Ping Li, Chun-Ping Wan, Ze-Wei Mao

引用次数: 0

Abstract

Ulcerative colitis (UC) is a chronic, nonspecific inflammatory bowel disease that is very difficult to cure. In this study, we have designed and synthesized a series of new 1,2,3-triazole-linked (±)-Agrimonolide derivatives and evaluated their anti-inflammatory activities. The in vitro results demonstrated that most triazole derivatives effectively inhibited NO production, and most compounds exhibited better anti-inflammatory activity than that of (±)-Agrimonolide and positive drug Dexamethasone. The further in vivo tests indicated that 6d could inhibit the release of inflammatory mediators in the colon tissue and alleviate Ulcerative colitis by inhibiting JAK1/STAT3 pathways.

查看原文本刊更多论文

新的1,2,3-三唑连接（±）-农单内酯衍生物作为抗溃疡性结肠炎药物抑制JAK1/STAT3途径。

溃疡性结肠炎（UC）是一种慢性、非特异性炎症性肠病，很难治愈。在本研究中，我们设计并合成了一系列新的1,2,3-三唑（±）-农单内酯衍生物，并对其抗炎活性进行了评价。体外实验结果表明，大多数三唑类化合物均能有效抑制NO的产生，且大多数化合物的抗炎活性优于（±）-Agrimonolide和阳性药物地塞米松。进一步的体内实验表明，6d可以通过抑制JAK1/STAT3通路，抑制结肠组织中炎症介质的释放，缓解溃疡性结肠炎。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Molecular Diversity 化学-化学综合

CiteScore

7.30

自引率

7.90%

发文量

219

审稿时长

2.7 months

期刊介绍： Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;