期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 11, 页码 5243-5250出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.08.043
关键词
Pyrrole derivatives; pyrrolo[2,3-d]pyrimidines; Pyrrolotriazolopyrimidines, pyrrolotetrazolopyrimidines; Synthesis; Docking studies; MIC; Antimicrobial
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.
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