Synthesis and Antimicrobial Evaluation of Novel Hydrazones and 1,3,4-Oxadiazoles Incorporating Bumetanide Derivatives

Salem, Ibrahim Mostafa; Mostafa, Samia M.; El-Sabbag, Osama I.; Ibrahim, Tarek S.; Abdulrahmanf, Ahmed; Bendary, Mahmoud M.

doi:10.21608/rpbs.2018.23373

Synthesis and Antimicrobial Evaluation of Novel Hydrazones and 1,3,4-Oxadiazoles Incorporating Bumetanide Derivatives

Document Type : Original Article

Authors

¹ Pharmaceutical Chemistry Departement, Faculty of Pharmacy, Suez Canal University

² Pharmaceutical Chemistry Department, Suez Canal University, Faculty of Pharmacy, Ismailia, Egypt

³ Medicinal Chemistry Department, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.

⁴ Pharmaceutical Chemistry Department, Faculty of Pharmacy, Taif University, Taif, Saudi Arabia

⁵ Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt.

⁶ Department of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah, 21589, Saudi Arabia.

⁷ Department of Pharmaceutical chemistry, Faculty of Pharmacy, Port Said University, Port Said, Egypt

⁸ Department of Microbiology and Immunology, Faculty of Pharmacy, Port Said University, Port Said, Egypt

10.21608/rpbs.2018.23373

Abstract

The aim of this study is to synthesize new benzenesulfonamide derivatives that possess antibacterial activity using Bumetanide as a precursor of benzenesulfonamide. A novel series of hydrazones containing benzenesulfonamides (4a-i) and 1,3,4 oxadiazole containing benzenesulfonamides (5a-e) were prepared and their antibacterial and antifungal activities were measured using microplate broth assay against Gram-positive: Staphylococcus aureus, Gram-negative: Escherichia coli and Pseudomonas aeruginosa and Fungi: Aspergillus fumigates and Candida albicans. The results showed that some of the prepared compounds exhibit a good to excellent activity against the mentioned bacteria, however all the series showed no activity against fungi. Among the series, Compound (4i) demoed an excellent antibacterial activity better than that of the standard reference (Sulfamethoxazole) against Escherichia coli, while compounds (4c, 4e, 4g) showed good activity against all tested bacterial strains equals to Sulfamethoxazole activity. Moreover, compounds (4g, 5d) exert an antimicrobial activity equals to that of Sulfamethoxazole against Pseudomonas aeruginosa, while compounds (4a, 4b, 4c, 4f, 4g, 4h) exhibit similar activity to Sulfamethoxazole against Escherichia coli.

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