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Antibacterial, Antifungal and Cytotoxic Evaluation of Some New Quinazolinone Derivatives



Hassanzadeh F1 ; Jafari E1 ; Hakimelahi GH1, 2 ; Rahmani Khajouei M1 ; Jalali M3 ; Khodarahmi GA1
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Institute of Chemistry, Academia Sinica, Nankang, Taipei, Taiwan
  3. 3. Department of Nutrition, School of Health, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Research in Pharmaceutical Sciences Published:2012

Abstract

Quinazolinone ring system is renown because of its wide spectrum of pharmacological activities due to various substitutions on this ring system. In this study, the minimum inhibitory concentration of the synthesized compounds in our laboratory was determined by micro dilution Alamar Blue® Assay against six strains of bacteria (three Gram-positive and three Gram-negative) and three strains of fungi. Following a broth micro dilution minimum inhibitory concentration (MIC) test, Minimum Bactericidal Concentration (MBC) and Minimum Fungicidal Concentration (MFC) tests were performed. Cytotoxic effects of the compounds were measured using the MTT colorimetric assay on HeLa cell line. Results of antimicrobial screening showed that compounds had better bacteriostatic activity against Gram-negative bacteria. Results from MBC revealed that these compounds had more significant bacteriostatic than bactericidal activities. Nearly all screened compounds showed good activity against C. albicans and A. niger. Results from MFC indicated that these compounds had better fungistatic rather than fungicidal activities. The synthesized target molecules were found to exhibit different cytotoxicity in the range of 10 to 100 μM on HeLa cell line. Compounds 6 and 7 exhibited acceptable cytotoxicity approximately 50% at 10 μM concentration.
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