Synthesis and Antibacterial Activity of 4-Aryl-2-(1-substituted ethylidene)thiazoles
作者： Alaa A. Hassan , Yusria R. Ibrahim , Essmat M. El-Sheref , Mohamed Abdel-Aziz , Stefan Bräse
关键词: Penicillin 、 Aryl 、 Bacteria 、 Minimum inhibitory concentration 、 Staphylococcus aureus 、 Chemistry 、 Ciprofloxacin 、 Sulbactam 、 Stereochemistry 、 Medicinal chemistry 、 Antibacterial activity
摘要: (E)-4-Aryl-2-[2-(1-substituted ethylidene)hydrazinyl]thiazoles and (Z)-3-substituted-4-aryl-2-[(E)-(1-phenylethylidene)hydrazono]-2,3-dihydrothiazoles were synthesized by the reaction of (substituted ethylidene)hydrazinecarbothioamides with ω-bromoacetophenones. The characterization this new class compounds was performed using different spectroscopic tools. structure (Z)-3-benzyl-4-(4-bromophenyl)-2-[(E)-(1-phenylethylidene)hydrazono]-2,3-dihydrothiazole 6e unambiguously confirmed single-crystal X-ray crystallography. Compounds 5a-e, 5i, 6e, 6g, 6i screened for their in vitro antibacterial activity against strains microorganisms; most tested exhibited promising some organisms compared to ciprofloxacin sulbactam penicillin. 5e, several-fold significant Gram-positive bacteria Staphylococcus aureus, better than ciprofloxacin, minimum inhibitory concentration values ranging from 0.05 0.4 µg/mL. rest gave activities Gram-negative bacterial strains.
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