Synthesis and in Vitro Antimicrobial and Cytotoxicity Activities of 2-[(2-nitro-1-phenylalkyl)thio]benzoic Acid Derivatives

Authors: MEHTAP GÖKÇE, SEMRA UTKU, ERDOĞAN BERÇİN, BERRİN ÖZÇELİK, TANER KARAOĞLU, NİNGUR NOYANALPAN

Abstract: In this research 14 compounds were tested for their antimicrobial activity. The synthesis of 7 compounds corresponding to 2-[(2-nitro-1-phenyl-propyl)thio]benzoic acids 4 has not been reported before and 7 compounds corresponding to 2-[(2-nitro-1-phenyl-ethyl) thio]benzoic acid 3 were reported by our research group. The antibacterial activity of the title compounds was evaluated by 2 Gram (+) (Staphylococcus aureus, Bacillus subtilis) and 2 Gram (-)(Pseudomonas aeruginosa, Escherichia coli) microorganisms. The antifungal activity of the compounds was also determined against yeast-like fungi (Candida albicans, C. krusei). For antibacterial activity, ampicillin and for antifungal activity, fluconazole and ketoconazole have been used as reference compounds. All of the 2-[(2-nitro-1-phenyl-ethyl)thio]benzoic acid 3 derivatives were more active than the reference compound ketoconazole in the antifungal activity test. The title compounds were also screened by consecutive dilution to explore their toxicity to a Vero cell line. Except for 3d and 3e all of the compounds 3 exhibited lower toxicity than ketoconazole.

Keywords: 2-[(2-nitro-1-phenylalkyl)thio]benzoic acid derivatives, \beta-Nitrostyrenes, Antibacterial Activity, Antifungal Activity, Cytotoxic Activity

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