Synthesis and evaluation of novel 2,4-disubstituted arylthiazoles against T. brucei,RSC Medicinal Chemistry

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Synthesis and evaluation of novel 2,4-disubstituted arylthiazoles against T. brucei
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2019/12/19 , DOI: 10.1039/c9md00478e
Markos-Orestis Georgiadis ₁ , Violeta Kourbeli ₁ , Ioannis P Papanastasiou ₁ , Andrew Tsotinis ₁ , Martin C Taylor ₂ , John M Kelly ₂

Affiliation

The design, synthesis and pharmacological evaluation of the 4-substituted-2-[3-(adamant-1-yl)-4-fluorophenyl]thiazoles 1a–j, the 4-substituted-2-[4-(adamant-1-yl)phenyl]thiazoles 2a–h, the 2-substituted-4-[4-(adamant-1-yl)phenyl]thiazoles 3a–e, the N-substituted 2-phenylthiazol-4-ethylamides 4a, b and the N-substituted 4-phenylthiazol-2-ethylamides 4c, d is described. Compounds 1a and 2a exhibit trypanocidal activity in the range of IC₅₀ = 0.42 μM and IC₅₀ = 0.80 μM, respectively. Both of these derivatives bear a lipophilic end, which consists of a 4-(1-adamantyl) phenyl or a 3-(1-adamantyl)phenyl moiety, a 1,3-thiazole ring and a functional end, which comprises of an alkylamine and can be considered as promising candidates for the treatment of Trypanosoma brucei infections.

中文翻译：

新型 2,4-二取代芳基噻唑抗布氏杆菌的合成与评价

4-取代-2-[3-(adamant-1-yl)-4-氟苯基]噻唑1a-j、4-取代-2-[4-(adamant-1- )的设计、合成和药理学评价基）苯基]噻唑2a-h，2-取代的-4-[4-（金刚烷-1-基）苯基]噻唑3a-e，N-取代的 2-苯基噻唑-4-乙基酰胺4a，b和N描述了-取代的4-苯基噻唑-2-乙基酰胺4c、d。化合物1a和2a在 IC ₅₀ = 0.42 μM 和 IC ₅₀范围内表现出杀锥虫活性= 0.80 μM，分别。这两种衍生物都带有亲脂性末端，由 4-(1-金刚烷基) 苯基或 3-(1-金刚烷基) 苯基部分、1,3-噻唑环和由烷基胺组成的官能末端组成并且可以被认为是治疗布氏锥虫感染的有希望的候选者。

更新日期：2020-02-13

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