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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

1
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia
2
Department of Chemistry, College of Sciences, Hail University, P.O. Box 2440, Hail 81451, Saudi Arabia
3
Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia 21321, Alexandria, Egypt
4
King Abdulaziz City for Science and Technology, P.O. Box 6086, Riyadh-11442, Saudi Arabia
5
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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Abstract

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
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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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