Suppr超能文献

一种新型衍生物 4-{5-[4-(4-氨基-5-巯基-4H-[1,2,4]三唑-3-基)-苯基]-3-三氟甲基-吡唑-1-基}-苯磺酰胺的高效合成及其抗炎潜力。

An efficient method for the synthesis of novel derivatives 4-{5-[4-(4-amino-5-mercapto-4H-[1,2,4]triazol-3-yl)-phenyl]-3-trifluoromethyl-pyrazol-1-yl}-benzenesulfonamide and their anti-inflammatory potential.

机构信息

Department of Chemistry, Hafiz Hayat Campus, University of Gujrat, Gujrat, Pakistan.

Department of University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.

出版信息

Bioorg Chem. 2019 Oct;91:103110. doi: 10.1016/j.bioorg.2019.103110. Epub 2019 Jul 5.

Abstract

The present work describe the synthesis of a novel series of celecoxib derivatives (6a-m) and they were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV and IX which are involved in a variety of diseases such as glaucoma, retinitis pigmentosa, epilepsy and tumors etc. These compounds showed interesting inhibitory activity for these isoforms, with several low nanomolar derivatives identified against all these enzymes. The in-vivo anti-inflammatory activity of the synthesized compounds were evaluated using Celecoxib as reference standard by paw Oedema model on albino Wistar. Most of the compounds showed higher in-vivo anti-inflammatory activity compared to Celecoxib.

摘要

本工作描述了一系列新型塞来昔布衍生物(6a-m)的合成,并对其作为碳酸酐酶(CA,EC 4.2.1.1)抑制剂进行了评价,针对涉及多种疾病的人(h)同工型 hCA I、II、IV 和 IX,这些疾病包括青光眼、视网膜色素变性、癫痫和肿瘤等。这些化合物对这些同工酶表现出有趣的抑制活性,其中一些低纳摩尔衍生物对所有这些酶都有抑制作用。通过爪肿胀模型在白化 Wistar 大鼠上,以塞来昔布为参考标准,评价了合成化合物的体内抗炎活性。与塞来昔布相比,大多数化合物表现出更高的体内抗炎活性。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验