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

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Abstract

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.

Graphical abstract: Synthesis and evaluation of novel 2,4-disubstituted arylthiazoles against T. brucei

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Article information


Submitted
08 Oct 2019
Accepted
22 Nov 2019
First published
19 Dec 2019

This article is Open Access

RSC Med. Chem., 2020, Advance Article
Article type
Research Article

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

M. Georgiadis, V. Kourbeli, I. P. Papanastasiou, A. Tsotinis, M. C. Taylor and J. M. Kelly, RSC Med. Chem., 2020, Advance Article , DOI: 10.1039/C9MD00478E

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