Synthesis of some new urea and thiourea derivatives and evaluation of their antimicrobial activities

被引:28
|
作者
Gulkok, Yildiz [2 ]
Bicer, Tuba [2 ]
Onurdag, Fatma Kaynak [3 ]
Ozgen, Selda [3 ]
Sahin, Mustafa Fethi [1 ]
Dogruer, Deniz Songul [1 ]
机构
[1] Gazi Univ, Fac Pharm, Dept Pharmaceut Chem, TR-06330 Ankara, Turkey
[2] Deva Ilac, Cerkezkoy, Tekirdag, Turkey
[3] Gazi Univ, Fac Pharm, Dept Microbiol, TR-06330 Ankara, Turkey
关键词
Urea; thiourea; 2(3H)-benzoxazolone; antimicrobial activity; BIOLOGICAL EVALUATION; 2(3H)-BENZOXAZOLONE; RESISTANCE; INHIBITORS; POTENT; HIV;
D O I
10.3906/kim-1106-54
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In the present study, 18 new compounds were synthesized, 9 of which were urea (9a-e, 10a-d) while the others were thiourea (11a-e, 12a-d) derivatives. These derivatives were prepared by the reaction of 6-amino-5-nonsubstituted/chloro-3-methyl-2(3H)-benzoxazolones used as key intermediates with the appropriate isocyanates and isothiocyanates. The chemical structures of new compounds were confirmed by H-1-NMR, mass, and elemental analysis. The synthesized compounds were screened for their antibacterial and antifungal activities against some pathogenic strains. Compounds 9a, 9b, 9e, 10a, and 10c, urea derivatives, and compounds 12a and 12d, thiourea derivatives, exhibited a relatively good inhibitory profile against E. coli, with a MIC value of 32 mu g/mL when compared with the other target compounds.
引用
收藏
页码:279 / 291
页数:13
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