Volume 17, Issue 3 (9-2018)
TB 2018, 17(3): 77-85 |
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Tamaddon F, Moradi B, Nasiri A R, Rahbar F. Synthesis and in Vitro Evaluation of Antifungal and Antibacterial Activity of 2,3-dihydroquinazolinone Derivatives . TB 2018; 17 (3) :77-85
URL: http://tbj.ssu.ac.ir/article-1-2684-en.html
URL: http://tbj.ssu.ac.ir/article-1-2684-en.html
, ftamaddon@yazd.ac.ir
Abstract: (2658 Views)
Introduction: By development of bacterial drug-resistance to traditional antibacterial drugs and fungal infections, the need to design, synthesis, and use of new and effective antibacterial and antifungal drugs is increased. Quinazolinone derivatives are heterocyclic compounds with nitrogen atoms that have pharmacological properties such as anti-bacterial, anti-tumor, anti-inflammatory and antifungal properties. The aim of this study was to synthesize of new derivatives of dihydroquinazolinone and study of their anti-bacterial and antifungal properties.
Methods: This research is an experimental work in which four dihydroquinazolinone derivatives were synthesized, by a new environmental-safe method and identified by various spectroscopic methods. Antibacterial activities of these derivatives were investigated against Escherichia coli gram-negative, and bacillus subtilis gram-positive in comparesion with amikacin. Antifungal activities of these derivatives were investigated against Aspergillus niger fungus and compared with ketoconazole. Both of antifungal and antibacterial activities of these synthetic compounds derivatives was checked by disk diffusion method with measuring the zone inhibition.
Results: All synthetic dihydroquinazolinones that were synthesized in high yields and purity, showed good antibacterial and antifungal properties. The compound 1d 2-phenyl-2,3-dihydroquinazolin-4(1H)-one derivative of these compounds showed more antimicrobial activities and antifungal comparable with the Amikacin and Ketoconazole standard antibacterial and antifungal drugs.
Conclusion: Synthetic dihydroquinazolinone derivatives in this work have good antifungal and antibacterial activities. The higher antifungal and antibacterial activity of 2-phenyl-2,3-dihydroquinazolin-4(1H)-one derivative can be related to more hydrophobicity of the phenyl group as a substitution in position 2.
Methods: This research is an experimental work in which four dihydroquinazolinone derivatives were synthesized, by a new environmental-safe method and identified by various spectroscopic methods. Antibacterial activities of these derivatives were investigated against Escherichia coli gram-negative, and bacillus subtilis gram-positive in comparesion with amikacin. Antifungal activities of these derivatives were investigated against Aspergillus niger fungus and compared with ketoconazole. Both of antifungal and antibacterial activities of these synthetic compounds derivatives was checked by disk diffusion method with measuring the zone inhibition.
Results: All synthetic dihydroquinazolinones that were synthesized in high yields and purity, showed good antibacterial and antifungal properties. The compound 1d 2-phenyl-2,3-dihydroquinazolin-4(1H)-one derivative of these compounds showed more antimicrobial activities and antifungal comparable with the Amikacin and Ketoconazole standard antibacterial and antifungal drugs.
Conclusion: Synthetic dihydroquinazolinone derivatives in this work have good antifungal and antibacterial activities. The higher antifungal and antibacterial activity of 2-phenyl-2,3-dihydroquinazolin-4(1H)-one derivative can be related to more hydrophobicity of the phenyl group as a substitution in position 2.
Type of Study: Research |
Subject:
Special
Received: 2018/02/28 | Accepted: 2018/05/5 | Published: 2018/09/15
Received: 2018/02/28 | Accepted: 2018/05/5 | Published: 2018/09/15
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