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Журнал структурной химии/2015/№ 2/

STRUCTURE AND BIOLOGICAL EVALUATION OF (E)-5-BROMO-2-METHOXY4-((PHENYLIMINO)METHYL)PHENOL DERIVATIVES AS ANTIBACTERIAL AGENTS

Three (E)-5-bromo-2-methoxy-4-((phenylimino)methyl)phenol derivatives (1—3) are synthesized and characterized by elemental analysis and single-crystal X-ray diffraction. The antibacterial activities of compounds 1—3 against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus are evaluated by the MTT method.

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2015. 56, 2 UDC 541.6:548.737 STRUCTURE AND BIOLOGICAL EVALUATION OF (E)-5-BROMO-2-METHOXY4-((PHENYLIMINO)METHYL)PHENOL DERIVATIVES AS ANTIBACTERIAL AGENTS W. Zhou, J. Ma, R.-J. Yuan, X. Han, H.-G. Liu, H.-L. Zhu School of Life Sciences, Shandong University of Technology, ZiBo 255049, P. R. China Email: hailiang_zhu@163.com (H.-L. Zhu) Received July, 20, 2013 Revised — November, 4, 2013 Three (E)-5-bromo-2-methoxy-4-((phenylimino)methyl)phenol derivatives (1—3) are synthesized and characterized by elemental analysis and single-crystal X-ray diffraction. <...> The antibacterial activities of compounds 1—3 against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus are evaluated by the MTT method. <...> INTRODUCTION Although several classes of antibacterial agents are presently available, resistance to these drugs constantly emerges in most of the pathogenic bacteria. <...> In order to prevent this serious medical problem, the elaboration of new types of antibacterial agents is a very important task [ 1 ]. <...> Apart of its flavor qualities, vanillin exhibits the antimicrobial potential and has been used as a natural food preservative [ 2 ]. <...> Schiff bases, named after Hugo Schiff [ 3 ], have also been shown to exhibit a broad range of biological activities, including antifungal, antibacterial, anti-malarial, antiproliferative, anti-inflammatory, antiviral, and antipyretic properties [ 4—12]. <...> The molecular hybridization approach is one of the most valuable structural modification tools useful for the discovery of ligands and prototypes presenting either optimized affinity for one bioreceptor or the ability to modulate more than one bioreceptor associated with the target disease [ 13 ]. <...> Hence, the impressive results of vanillin derivatives and various phenylamine fueled our interest in combining two scaffolds and exploring their possibilities as antibacterial agents. <...> The crystal structures of compounds (1—3) were determined. <...> General synthesis method of (E)-5-bromo-2-methoxy-4-((phenylimino)methyl)phenol derivatives (1—3). <...> The organic layer was filtered, and concentrated under reduced pressure to give the pure compound a. <...> After cooling in the air, the resultant solid was filtered, washed with water, and dried to give the compound c. The equivocal compound c and substituted aromatic amine <...>
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