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Molecules 2014, 19(7), 8725-8739; doi:10.3390/molecules19078725

Synthesis, Anti-microbial and Molecular Docking Studies of Quinazolin-4(3H)-one Derivatives

Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
Department of Chemistry, College of Sciences, Hail University, P.O. Box 2440, Hail 81451, Saudi Arabia
Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia 21321, Alexandria, Egypt
King Abdulaziz City for Science and Technology, P.O. Box 6086, Riyadh-11442, Saudi Arabia
Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75210, Pakistan
Authors to whom correspondence should be addressed.
Received: 15 April 2014 / Revised: 6 June 2014 / Accepted: 9 June 2014 / Published: 25 June 2014
(This article belongs to the Section Organic Synthesis)
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In this work, synthesis, antimicrobial activities and molecular docking studies of some new series of substituted quinazolinone 2ah and 3ad were described. Starting form 2-aminobenzamide derivatives 1, a new series of quinazolinone derivatives has been synthesized, in high yields, assisted by microwave and classical methods. Some of these substituted quinazolinones were tested for their antimicrobial activity against Gram-negative bacteria (Pseudomonas aeruginosa and Esherichia coli) and Gram-positive bacteria (Staphylococcus aureus, and Bacillus subtilis), and anti-fungal activity against (Aspergillus fumigatus, Saccharomyces cervevisiae, and Candida albicans) using agar well diffusion method. Among the prepared products, 3-benzyl-2-(4-chlorophenyl)quinazolin-4(3H)-one (3a) was found to exhibits the most potent in vitro anti-microbial activity with MICs of 25.6 ± 0.5, 24.3 ± 0.4, 30.1 ± 0.6, and 25.1 ± 0.5 µg/mL against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa and Esherichia coli, respectively. Compound 3a was found to exhibits the most potent in vitro anti-fungal activity with MICs of 18.3 ± 0.6, 23.1 ± 0.4, and 26.1 ± 0. 5 µg/mL against Aspergillus fumigatus, Saccharomyces cervevisiae, and Candidaal bicans, respectively. View Full-Text
Keywords: quinazolinone; antimicrobial agents; streptomycin; clotrimazole; molecular docking quinazolinone; antimicrobial agents; streptomycin; clotrimazole; molecular docking

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Mabkhot, Y.N.; Al-Har, M.S.; Barakat, A.; Aldawsari, F.D.; Aldalbahi, A.; Ul-Haq, Z. Synthesis, Anti-microbial and Molecular Docking Studies of Quinazolin-4(3H)-one Derivatives. Molecules 2014, 19, 8725-8739.

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