Synthesis, computational evaluation and pharmacological assessment of acetylsalicylic esters as anti-inflammatory agents

Mancuso, Raffaella; Ferlazzo, Nadia; Luca, Giorgio De; Amuso, Roberta; Piccionello, Antonio Palumbo; Giofrè, Salvatore V.; Navarra, Michele; Gabriele, Bartolo

doi:10.1007/s00044-018-02284-3

Cited by 1 publication

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“…如水杨酸 C(1)-COOH 与相应的醇酯化生成衍生物 10a 和 10b (Scheme 5), 两者能够抑制 NMDA 引起的神经毒性 [16] . 将 C(1)-COOH 与戊醇、己醇、癸醇及十四醇酯化后, 再将酚羟基酰化得到衍生物 11a～11d (Scheme 5), 化合物 11a～11c 在体外实验中显示出与阿司匹林相同的抗炎活性 [17] . 氧化应激与炎症的产生是与年龄相关的机体功能下降的主要影响因素, 阿司匹林可通过减少类胰岛素信号的释放, 从而防止氧化应激, 延缓与年龄相关的机体功能衰退, 达到抗衰老的作用 [18,19] .…”

Section: 阿司匹林的骨架衍生与生物活性unclassified

Advances in the Study of Structural Modification of Aspirin and Their Biological Activities

Zhang¹,

Gao²,

Zhang³

et al. 2020

Chin. J. Org. Chem.

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Aspirin (ASP), the first synthetic drug, is widely used as a non steroidal anti-inflammatory drug. It displays a variety of biological activities, such as anti-thrombosis, anti-inflammatory, anti-tumor, etc. A lot of works about the synthesis and related activity evaluation of its derivatives were reported. There are four kinds of derivatization methods: skeleton derivatization, prodrug derivatization, twin derivatization and metal coordination derivatization. According to the different modification sites, skeleton derivatization could be further divided into C(1)-COOH site modification, C(1)-COOH site and C(2)-OAc site simultaneous modification, C(2)-OAc site modification and benzene ring modification. NO-ASP is the main method to prepare antithrombotic derivatives, and metal coordination modification is the main synthesis scheme of anticancer derivatives. The structure modification and bioactivity research of aspirin in recent twenty years and the synthetic routes of 353 aspirin derivatives and the pharmacological activities of some derivatives are described, which provides a reference for the further development of aspirin derivatives.

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Section: 阿司匹林的骨架衍生与生物活性unclassified