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Synthesis and antibacterial activity of novel benzothiazole derivatives

Infectious diseases caused by bacteria affect millions of people and represent one of leading causes of death worldwide. On the other side, resistance of pathogenic bacteria to existing antibacterial drugs presents an additional problem. Therefore, the design of new compounds has become one of the most important areas of antibacterial research today. Benzothiazole and their heterocyclic derivatives represent an important class of compounds possessing a wide spectrum of biological activities such as antitumor, antimicrobial, antidiabetic, anti- inflammatory, anticonvulsant, antiviral, antioxidant, antitubercular, antimalarial, photosensitizing, diuretic, analgesic and other activities [1, 2]. Furthermore, benzothiazole–1, 2, 3-triazole–coumarin hybrid showed anti-Moraxella catarrhalis potency (MIC ≤ 0.25 μg cm-3) comparable to that of the reference antibiotic azithromycin [3].In order to evaluate their antibacterial activity, the novel 2-aryl-benzothiazole derivatives have been synthesized. Of the all evaluated compounds against Gram-positive bacteria (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative bacteria (Klebsiella pneumoniae, Escherichia coli and Pseudomonas aeruginosa) benzothiazole derivatives with N, N- diethylamine substituent showed the strongest activity against gram-negative clinical strains resistant to antibiotics compared to standard drug amikacin. [1] F.L. Gouveia et al., Eur J Med Chem 44 (2009) 2038. [2] R. S. Keri et al., Eur. J Med Chem 89 (2015) 207. [3] S. Maračić et al., Bioorg Med Chem 23(2015) 7448.

benzothiazole, click reaction, 1, 2, 3-triazole, antibacterial activity

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