Antibacterial, antifungal and cytotoxic evaluation of some new 2,3-disubstituted 4(3H)-quinazolinone derivatives

• Published in: Research in pharmaceutical sciences Vol. 7; no. 3; pp. 151 - 158
• Main Authors: Khodarahmi, G A, Khajouei, M Rahmani, Hakimelahi, G H, Abedi, D, Jafari, E, Hassanzadeh, F
• Format: Journal Article
• Language: English
• Published: Iran Medknow Publications & Media Pvt Ltd 01.07.2012
• Subjects: Original; Cytotoxicity; Antifungal; 4(3H)-Quinazolinone; Antibacterial
• ISSN: 1735-5362; 1735-9414

In this study antibacterial, antifungal and cytotoxic effects of some new 2,3-disubstituted 4(3H)-quinazolinone derivatives have been evaluated. The in vitro antibacterial and antifungal tests of new synthesized compounds were performed using MABA method against six strains of bacteria (three Grampositive and three Gram-negative) and three strains of fungi. Also Minimum Bactericidal Concentration (MBC) and Minimum Fungicidal Concentration (MFC) tests were performed. All synthesized compounds indicated mild antibacterial effects especially against Gram-negative bacteria. The most sensitive bacteriumwas E. coli. All strains of tested fungi were sensitive to the synthesized compounds mostly at 32 μg/ml and there was no significant differences in the sensitivity of the tested compounds. MBC and MFC data indicated that tested compounds act as bactriostatic and fungistatic agents. Cytotoxic activity of the compounds was screened at 1, 10 and 100 μM concentrations against HeLa cells using the MTT colorimetric assay. While the synthesized compounds did not show significant cytotoxic activities, compounds 7a(3) and 7a(4) reduced cell viability to about 50% at 100 μM concentration. The present study revealed that most of the new synthesized compounds possess good antifungal effects and they could be considered as valuable candidates for further structural modification to design more potent antifungal agents.