Back to Archived Journals » Research and Reports in Medicinal Chemistry » Volume 6

Synthesis, characterization, antitubercular and antibacterial activity, and molecular docking of 2,3-disubstituted quinazolinone derivatives

Authors Komarla R, Nizamuddin ND, Surur A, Mekonnen YT

Received 30 June 2015

Accepted for publication 23 January 2016

Published 11 May 2016 Volume 2016:6 Pages 15—26


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3

Editor who approved publication: Dr Xing-Cong Li

Video abstract presented by Abdrrahman Shemsu Surur.

Views: 492

KK Rajasekhar,1 ND Nizamuddin,1 Abdrrahman Shemsu Surur,2 Yenus Tadesse Mekonnen2

1Department of Pharmaceutical Chemistry, Sri Padmavathi School of Pharmacy, Tiruchanur, India; 2Department of Pharmaceutical Chemistry, School of Pharmacy, College of Medicine and Health Sciences, University of Gondar, Gondar, Ethiopia

Abstract: Quinazolinone derivatives, which are known for their versatile biological activities, have been reported to show significant antibacterial and antitubercular activities. Fourteen compounds that belong to either 2-methyl substituted quinazolinone or 2-phenyl substituted quinazolinones were synthesized. Compounds 5a–e and 8a–c showed a minimum inhibitory concentration value between 6.25 and 100 µg/mL against Mycobacterium tuberculosis. Compounds 5g and 8d, on the other hand, showed significant antibacterial activity against Staphylococcus albus and Streptococcus pyogenes. The use of amido, thioamido, imidamido, N,N-dimethyl guanidinyl, or N-pyridoyl substituents at 3-position of quinazolinone was found to increase antitubercular activity. A binding affinity prediction by autodock vina was higher for the 2-phenyl series, which may be due to increased hydrophobic interactions within the binding site of enoyl-acyl carrier protein reductase.

Keywords: quinazolinones, antitubercular activity, antibacterial activity, autodock vina

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]