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更新于：2025-05-07

Fentiazac

芬替酸

更新于：2025-05-07

概要

基本信息

药物类型

小分子化药

别名

4-(4-Chlorophenyl)-2-phenyl-5-thiazoleacetic acid、4-(p-Chlorophenyl)-2-phenyl-5-thiazoleacetic acid、Fentiazac (JAN/USAN/INN)

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靶点-

作用方式-

作用机制-

治疗领域

神经系统疾病其他疾病

在研适应症

炎症疼痛

非在研适应症-

原研机构-

在研机构-

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C17H12ClNO2S

InChIKeyJIEKMACRVQTPRC-UHFFFAOYSA-N

CAS号18046-21-4

关联

100 项与芬替酸相关的临床结果

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100 项与芬替酸相关的转化医学

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100 项与芬替酸相关的专利（医药）

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168

项与芬替酸相关的文献（医药）

2025-01-23·Nature

Photochemical permutation of thiazoles, isothiazoles and other azoles

Article

作者: Dos Santos, Thiago ; Yildiz, Dilara Berna ; Buettner, Cornelia S ; Ruffoni, Alessandro ; Xu, Yan ; Derdau, Volker ; Buettner, Cornelia S. ; Bossart, Martin ; Lonardi, Giovanni ; Alonso, Maialen ; Roure, Baptiste ; Leonori, Daniele ; dos Santos, Thiago ; Méndez, María ; Llaveria, Josep

Thiazoles and isothiazoles are privileged motifs in drug and agrochemical discovery^1,2. The synthesis of these derivatives is generally approached, designed and developed on a case-by-case basis. Sometimes, the lack of robust synthesis methods to a given target can pose considerable difficulties or even thwart the preparation of specific derivatives for further study^3,4. Here we report a conceptually different approach in which photochemical irradiation can be used to alter the structure of thiazoles and isothiazoles in a selective and predictable manner. On photoexcitation, these derivatives populate their π,π* singlet excited states that undergo a series of structural rearrangements, leading to an overall permutation of the cyclic system and its substituents. This means that once the initial heteroaromatic scaffold has been prepared, it can then function as an entry point to access other molecules by selective structural permutation. This approach operates under mild photochemical conditions that tolerate many chemically distinct functionalities. Preliminary findings also show the potential for extending this method to other azole systems, including benzo[d]isothiazole, indazole, pyrazole and isoxazole. This strategy establishes photochemical permutation as a powerful and convenient method for the preparation of complex and difficult-to-access derivatives from more available structural isomers.

2021-07-16·Chemistry – A European Journal

“Snapshot” Trapping of Multiple Transient Azolyllithiums in Batch

Article

作者: Okano, Kentaro ; Feng, Yuxuan ; Mori, Atsunori ; Inoue, Kengo

AbstractRecent developments in flow microreactor technology have allowed the use of transient organolithium compounds that cannot be realized in a batch reactor. However, trapping the transient aryllithiums in a “halogen dance” is still challenging. Herein is reported the trapping of such short‐lived azolyllithiums in a batch reactor by developing a finely tuned in situ zincation using zinc halide diamine complexes. The reaction rate is controlled by the appropriate choice of diamine ligand. The reaction is operationally simple and can be performed at 0 °C with high reproducibility on a multigram scale. This method was applicable to a wide range of brominated azoles allowing deprotonative functionalization, which was used for the concise divergent syntheses of both constitutional isomers of biologically active azoles.

2020-11-20·Current Topics in Medicinal Chemistry4区 · 医学

2,4,5-Trisubstituted Thiazole: A Privileged Scaffold in Drug Design and Activity Improvement

4区 · 医学

Review

作者: Shu, Bing ; Zhang, Yaodong ; Deora, Girdhar Singh ; Li, Qing-Shan ; Zhang, Zhen

Thiazole is an important 5-membered heterocyclic compound containing nitrogen and sulfur atoms with various pharmaceutical applications including anti-inflammatory, anti-cancer, anti-viral, hypoglycemic, anti-bacterial and anti-fungal activities. Until now, the FDA-approved drugs containing thiazole moiety have achieved great success such as dasatinib and dabrafenib. In recent years, considerable research has been focused on thiazole derivatives, especially 2,4,5-trisubstituted thiazole derivatives, due to their multiple medicinal applications. This review covers related literature in the past 20 years, which reported the 2,4,5-trisubstituted thiazole as a privileged scaffold in drug design and activity improvement. Moreover, this review aimed to provide greater insights into the rational design of more potent pharmaceutical molecules based on 2,4,5-trisubstituted thiazole in the future.

100 项与芬替酸相关的药物交易

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