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Int. J. Mol. Sci. 2015, 16(4), 8719-8743;

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

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
Department of Applied Organic Chemistry, National Research Centre, Dokki, Cairo 12622, Egypt
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
Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo 11754, Egypt
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: José Alberto Pereira
Received: 13 February 2015 / Revised: 2 April 2015 / Accepted: 8 April 2015 / Published: 20 April 2015
(This article belongs to the Section Biochemistry)
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In continuation of our endeavor towards the development of potent and effective antimicrobial agents, three series of halophenyl bis-hydrazones (14an, 16ad, 17a and 17b) 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. View Full-Text
Keywords: synthesis; antimicrobial activity; halophenyl bis-hydrazones; antimycobacterial; 2D-QSAR synthesis; antimicrobial activity; halophenyl bis-hydrazones; antimycobacterial; 2D-QSAR

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Abdel-Aziz, H.A.; Eldehna, W.M.; Fares, M.; Al-Rashood, S.T.A.; Al-Rashood, K.A.; Abdel-Aziz, M.M.; Soliman, D.H. Synthesis, Biological Evaluation and 2D-QSAR Study of Halophenyl Bis-Hydrazones as Antimicrobial and Antitubercular Agents. Int. J. Mol. Sci. 2015, 16, 8719-8743.

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