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

被引:1
|
作者
Khodarahmi, Ghadamali [1 ,2 ]
Jafari, Elham [1 ]
Hakimelahi, Gholamhossein [1 ,3 ]
Abedi, Daryoush [4 ]
Khajouei, Marzieh Rahmani [1 ]
Hassanzadeh, Farshid [1 ,2 ]
机构
[1] Isfahan Univ Med Sci, Fac Pharm & Pharmaceut Sci, Dept Med Chem, Esfahan, Iran
[2] Isfahan Pharmaceut Sci Res Ctr, Esfahan, Iran
[3] Acad Sinica, Inst Chem, Taipei, Taiwan
[4] Isfahan Univ Med Sci, Fac Pharm & Pharmaceut Sci, Dept Microbiol, Esfahan, Iran
来源
关键词
Fused quinazolinons; Deoxyvasicinone; Benzoxazinone; Antibacterial activity; Antifungal activity; AZA-WITTIG REACTION; DEOXYVASICINONE; MACKINAZOLINONE; TRYPTANTHRIN; INHIBITORS;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:789 / 797
页数:9
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