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Title: Design and synthesis of novel 2,4,5-thiazole derivatives as 6-APA mimics and antimicrobial activity evaluation
Authors: Nuha, Demokrat
Evren, Asaf Evrim
Yılmaz Cankılıç, Meral
Yurttaş, Leyla
Keywords: Thiazole
antibacterial activity
antifungal activity
physicochemical property prediction
Issue Date: 2021
Publisher: Taylor & Francis Ltd
Abstract: Nine new thiazole derivatives were synthesized considering 6-acetyl penicillanic acid (6-APA) and investigated for their antimicrobial activity. Ethyl 2-(2-mercaptoacetamido)-4-methylthiazole-5-carboxylate derivatives (3a-3i) were gained with a two-step synthetic method using conventional Hantzsch thiazole synthesis. The structural elucidation of the compounds was performed by H-1-NMR, C-13-NMR spectral data and HRMS. All compounds were tested on eleven bacteria and sixteen fungi species and minimum inhibitory concentration (MIC) was determined for each. Compounds 3d (4-methyl-2-(2-((5-methyl-1,3,4-thiadiazol-2-yl), 3f (4-methyl-2-(2-((5-nitro-1H-benzimidazol-2-yl) and 3g (4-methyl-2-(2-((5-methyl-4H-1,2,4-triazol-3-yl) bearing thiazole, 5-nitrobenzimidazole and triazole rings respectively exhibited high antimicrobial activity against most of the strains. In silico physicochemical properties were calculated for the compounds and it was detected that they comply with the rules of drug availability.
ISSN: 1042-6507
Appears in Collections:İstatistik Bölümü Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu
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