Synthesis and Biological Assessment of New Thiazoles for Mycobacterial Infections and Biofilm Disruption
Year: 2025
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide Sixteen thiazoles, of which nine are unprecedented substances ( 11, 12, 15, 16, 17, 19, 20, 23, and 24 ), were obtained by a cyclocondensation reaction between a thioamide and an α-bromoketone, via Hantzsch synthesis. All thiazoles ( 11 – 26 ), along with four thiosemicarbazone derivatives ( 7 – 10 ) and their precursors ( 1 – 6 ), were evaluated for their activity against Mycobacterium species Mycobacterium abscessus, Mycobacterium massiliense, Mycobacterium fortuitum, and Mycobacterium smegmatis, as well as for their antibiofilm properties. Among them, compounds 7, 8, 14, 17, 18, 19, 20, and 21 showed promising results in minimum inhibitory concentration (MIC) assays, demonstrating bactericidal activity within 48 h. Moreover, all these compounds inhibited biofilm formation. Notably, the unprecedented thiazole 17, along with 18 (MIC = 36 μmol L –1 ) and 21 (MIC = 65 μmol L –1 ), exhibited the lowest MIC values against all tested species, outperforming the reference drugs. Furthermore, these compounds showed a high degree of selectivity toward mycobacterial cells, as confirmed by cytotoxicity assays using peripheral blood mononuclear cells (PBMC) and Vero cells. These findings highlight the strong antimycobacterial potential of the new thiazole derivatives, warranting further investigation.
Source: ACS Omega
Authors: Laís Regina dos Santos Folquitto, Fallon dos Santos Siqueira, Tayná Roberta Nunes, Thiago Belarmino de Souza, Diogo Teixeira Carvalho, Rafael Pereira Machado, Antonio Carlos Doriguetto, Marli Matiko Anraku De Campos, Livia de Figueiredo Diniz, Marisi Gomes Soares, Daniela Aparecida Chagas de Paula, Danielle Ferreira Dias
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,935
Awards: AVANÇO DA PESQUISA E PÓS-GRADUAÇÃO NA UNIFAL-MG ATRAVÉS DA CRIAÇÃO DE REDES DE COLABORAÇÃO INTERNACIONAIS, DESENVOLVIMENTO DE NOVOS AZÓIS INIBIDORES DA PRODUÇÃO DE ERGOSTEROL DE FUNGOS: CANDIDATOS INOVADORES A FÁRMACOS ANTIFÚNGICOS, G2879888585, REDE MINEIRA DE PESQUISA E INOVAÇÃO EM QUÍMICA MEDICINAL - RMQM, G3594283485, G3690646728, G5115280995, FORTALECIMENTO DA INTERNACIONALIZAÇÃO ATRAVÉS DE REDES DE COLABORAÇÃO INTERNACIONAIS NA PESQUISA E PÓS-GRADUAÇÃO DA UNIFAL-MG, METABOLÔMICA DE CULTIVARES DE CAFÉ SUSCETÍVEIS E RESISTENTES À FERRUGEM (HEMILEIA VASTATRIX) E ANÁLISE DE VIABILIDADE ECONÔMICA: RELAÇÕES DA COMPOSIÇÃO QUÍMICA COM POTENCIAL ECONÔMICO, PERFIS DE RESISTÊNCIA E QUALIDADE SENSORIAL, SÍNTESE E AVALIAÇÃO DE HÍBRIDOS INSPIRADOS EM BENZOFURANOIDES NATURAIS: CONTRIBUIÇÃO À INOVAÇÃO E DESCOBERTA DE ANTIMICROBIANOS E MODULADORES DE RESISTÊNCIA, G7973128220, G8055969255, G8565212151, METABOLÔMICA, ISOLAMENTO DE SUBSTÂNCIAS DE ESPÉCIES VEGETAIS E SEMI-SÍNTESE DE DERIVADOS COM AÇÃO ANTI-INFLAMATÓRIA E DE NEUROPROTEÇÃO EM MODELO EXPERIMENTAL DA DOENÇA DE PARKINSON
OpenAlex ID: W4415323192