Synthesis of Some New Quinazolinone Derivatives and Evaluation of Their Antimicrobial Activities

نویسندگان

  • Daryoush Abedi Department of Microbiology, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
  • Elham Jafari Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
  • Farshid Hassanzadeh Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran. Isfahan Pharmaceutical Sciences Research Center, Isfahan, Iran.
  • Ghadamali Khodarahmi Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran. Isfahan Pharmaceutical Sciences Research Center, Isfahan, Iran.
  • Gholamhossein Hakimelahi Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran. Institute of Chemistry, Academia Sinica, Nankang, Taipei, Taiwan.
  • Marzieh Rahmani Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
چکیده مقاله:

Wide range of quinazolinone biological properties including: antibacterial, anticancer, and anti-inflammatory activities encouraged us to synthesis some fused quinazolinone derivatives. Anthranilic acid was condensed with chloro acylchloride followed by dehydration to form the benzoxazinone intermediate; subsequent addition of an amine provided the fused quinazolinones. Deoxyvasicinone which was previously synthesized by a multi step complex reactions was prepared in three steps using the following procedure: Log P values of the compounds were measured using the shake flask method in octanol/water solvent system. The synthesized compounds were evaluated against six strains of bacteria (three Gram-positive and three Gram-negative) and three strains of fungi. Overall results of antimicrobial tests showed that the compounds had better bacteriostatic activity against Gram-negative bacteria. The obtained results of MBC revealed that these compounds had more significant bacteriostatic than bactericidal activities. Almost all of the screened compounds showed good activity against C. albicans and A. niger. The obtained results of MFC indicated that these compounds had more significant fungistatic than fungicidal activities.

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synthesis of some new quinazolinone derivatives and evaluation of their antimicrobial activities

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عنوان ژورنال

دوره 11  شماره 3

صفحات  789- 797

تاریخ انتشار 2012-05-21

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