合成新型吡咯并[2,3-d]嘧啶衍生物作为抗菌和抗真菌剂。

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

机构信息

Department of Chemistry, Faculty of Science, Menufiya University, Shebin El-Kom, Egypt.

出版信息

Eur J Med Chem. 2010 Nov;45(11):5243-50. doi: 10.1016/j.ejmech.2010.08.043. Epub 2010 Aug 24.

DOI:10.1016/j.ejmech.2010.08.043

PMID:20828885

Abstract

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.

摘要

一系列新的吡咯衍生物、吡咯并[2,3-d]嘧啶衍生物、吡咯并三唑嘧啶和吡咯并四唑嘧啶被合成。对它们对金黄色葡萄球菌、大肠杆菌和白色念珠菌的抗菌活性进行了评价。吡咯并[2,3-d]嘧啶 3a-d、7a,e、11d 对白色念珠菌表现出优异的活性，MIC 为 0.31-0.62mg/mL。这些化合物的抗真菌活性优于标准药物（氟康唑，MIC 为 1.5mg/mL）。此外，吡咯并[2,3-d]嘧啶 3b,c、7e 对金黄色葡萄球菌表现出最好的活性，MIC 为 0.31mg/mL，优于标准药物（氨苄西林，MIC 为 0.62mg/mL）。其余化合物对细菌和真菌均无活性。