Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.,ACS Medicinal Chemistry Letters

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Design and Catalyzed Activation of Tak-242 Prodrugs for Localized Inhibition of TLR4-Induced Inflammation.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2020-01-03 , DOI: 10.1021/acsmedchemlett.9b00518
Michael A Plunk ₁ , Alyssa Alaniz ₂ , Olatunde P Olademehin ₁ , Thomas L Ellington ₁ , Kevin L Shuford ₁ , Robert R Kane _{1,

2}

Affiliation

Tak-242 (resatorvid), a Toll-like Receptor 4 (TLR4) inhibitor, has been identified as a potent suppressor of innate inflammation. As a strategy to target Tak-242 to select tissue, four TLR4-inactive prodrugs were synthesized for activation via two different release mechanisms. Two nitrobenzyl Tak-242 prodrugs released the parent drug upon exposure to the exogenous enzyme nitroreductase, while the two propargyl prodrugs were converted to Tak-242 in the presence of Pd0.

中文翻译：

Tak-242前药的设计和催化活化，用于TLR4诱导的炎症的局部抑制。

Tak-242（resatorvid）是Toll样受体4（TLR4）抑制剂，已被确定为先天性炎症的有效抑制剂。作为靶向Tak-242选择组织的策略，合成了四种TLR4失活的前药，通过两种不同的释放机制进行激活。两种硝基苄基Tak-242前药在暴露于外源酶硝基还原酶后释放了母体药物，而两种炔丙基前药在Pd0存在下转化为Tak-242。

更新日期：2020-01-08

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