SYNTHESIS AND EVALUATION OF NEW PHENYLTHIAZOLE DERVATIVES AS ANTIMICROBIAL AGENTS

Document Type : Original Article

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Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt

Abstract

The current arsenal of antimicrobials couldn't hold back the rapid and ferocious growth of the antimicrobial resistance phenomenon. Collectively the current situation points to the pressing need to develop other effective antimicrobial agents.
In the search for novel antimicrobials, phenylthiazole derivatives have recently been found to possess antibacterial activity particularly against a range of several antibiotic-resistant staphylococcus aureus strains. Modification of the nitrogenous head by incorporation the hydrolysable -HC=N- linkage within a pyrimidine ring bearing one or more hydrogen bond-promoting group led to the discovery of the second generation of phenylthiazoles, with more potent activity and longer half-lives compared to the lead compound 1a.
Based on the above rationale, the objective of this study was to create a new set of structures of n-butylphenylthiazole-5-pyrimidine that contains two or more heteroatoms in their side chain and to study the relationship between the structural form of these compounds and their antimicrobial activity and spectrum against certain multi-drug resistance (MDR) strains. The new set of derivatives is designed to cover all the possibilities of side chains carbon-units distance and spatial configurations.

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Al-Azhar Journal of Pharmaceutical Sciences
Volume 60, Issue 2 - Serial Number 2
September and October 2019
Pages 59-75

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