Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives as antibacterial and antifungal agents

被引:98
|
作者
Hilmy, Khalid Mohammed Hassan [1 ]
Khalifa, Maha M. A. [2 ]
Hawata, Mohammed Abd Allah [1 ]
Keshk, Reda Mohammed AboAlzeen [1 ]
El-Torgman, Abd Almeneam [1 ]
机构
[1] Menufiya Univ, Fac Sci, Dept Chem, Shibin Al Kawm, Egypt
[2] Al Azhar Univ, Fac Pharm, Dept Pharmaceut Chem, Cairo, Egypt
关键词
Pyrrole derivatives; pyrrolo[2,3-d]pyrimidines; Pyrrolotriazolopyrimidines; pyrrolotetrazolopyrimidines; Synthesis; Docking studies; MIC; Antimicrobial; PYRROLE;
D O I
10.1016/j.ejmech.2010.08.043
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of new pyrrole derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrrolotriazolopyrimidines and pyrrolotetrazolopyrimidines were synthesized. The evaluation of their antimicrobial activities against Staphylococcus aureus, Escherichia coli, and Candida albicans were carried out. Pyrrolo[2,3-d]pyrimidines 3a-d, 7a,e, 11d exhibited excellent activity against C albicans with MIC 0.31-0.62 mg/mL. These compounds displayed better antifungal activity than that of standard drug (fluconazole with MIC 1.5 mg/mL). Furthermore, pyrrolo[2,3-d]pyrimidines 3b,c, 7e exhibited the best activity against S. aureus with MIC 0.31 mg/mL, compared with the standard drug (ampicillin with MIC 0.62 mg/mL). The rest of the compounds were found to be inactive against bacteria and fungi. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:5243 / 5250
页数:8
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