Synthesis, Biological Evaluation and 2D-QSAR Study of Halophenyl Bis-Hydrazones as Antimicrobial andAntitubercular Agents

International Journal of Molecular Sciences

Sara T. A. Al-Rashood¹  Hatem A. Abdel-Aziz¹  Khalid A. Al-Rashood¹  Wagdy M. Eldehna²  Mohamed Fares²  Dalia H. Soliman²  Marwa M. Abdel-Aziz³ 

[1] Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University,P.O. Box 2457, Riyadh 11451, Saudi Arabia;Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Egyptian Russian University,Badr City, Cairo 11829, Egypt;The Regional Center for Mycology and Biotechnology, Al-Azhar University, Cairo 11759, Egypt;

关键词: synthesis;    antimicrobial activity;    halophenyl bis-hydrazones;    antimycobacterial;    2D-QSAR;   

DOI  :  10.3390/ijms16048719

来源: DOAJ

【 摘 要 】

In continuation of our endeavor towards the development of potent and effective antimicrobial agents, three series of halophenyl bis-hydrazones (14a–n, 16a–d, 17a and17b) were synthesized and evaluated for their potential antibacterial, antifungal and antimycobacterial activities. These efforts led to the identification of five molecules 14c, 14g, 16b, 17a and 17b (MIC range from 0.12 to 7.81 μg/mL) with broad antimicrobial activity against Mycobacterium tuberculosis; Aspergillus fumigates; Gram positive bacteria, Staphylococcus aureus, Streptococcus pneumonia, and Bacillis subtilis; and Gram negative bacteria, Salmonella typhimurium, Klebsiella pneumonia, and Escherichia coli. Three of the most active compounds, 16b, 17a and 17b, were also devoid of apparent cytotoxicity to lung cancer cell line A549. Amphotericin B and ciprofloxacin were used as references for antifungal and antibacterial screening, while isoniazid and pyrazinamide were used as references for antimycobacterial activity. Furthermore, three Quantitative Structure Activity Relationship (QSAR) models were built to explore the structural requirements controlling the different activities of the prepared bis-hydrazones.

【 授权许可】

Unknown