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Antibacterial, Antifungal and Cytotoxic Evaluation of Some New 2,3-Disubstituted 4(3H)-Quinazolinone Derivatives



Khodarahmi GA1, 2 ; Khajouei MR1 ; Hakimelahi GH1, 2, 3 ; Abedi D4 ; Jafari E1 ; Hassanzadeh F1, 2
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Isfahan Pharmaceutical Sciences Research Center, Isfahan, Iran
  3. 3. Institute of Chemistry, Academia Sinica, Nankang, Taipei, Taiwan
  4. 4. Department of Biotechnology and Isfahan Pharmaceutical Sciences Research Center, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Research in Pharmaceutical Sciences Published:2012

Abstract

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 7a3 and 7a4 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.
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