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Synthesis and antimicrobial evaluation of some new substituted purine derivatives.

Abstract：

:A series of 8,9-disubstituted adenines (4, 5, 8), 6-substituted aminopurines (10-13) and 9-(p-fluorobenzyl/cyclopentyl)-6-substituted aminopurines (16, 17, 19-30) have been prepared and the antimicrobial activities of these compounds against Staphylococcus aureus, methicillin-resistant S. aureus (MRSA, standard and clinical isolate), Bacillus subtilis, Escherichia coli and Candida albicans were evaluated. 6-[(N-phenylaminoethyl)amino]-9H-purine (12) which has no substitution at N-9 position and 9-cyclopentyl-6-[(4-fluorobenzyl)amino]-9H-purine (24) exhibited excellent activity against C. albicans with MIC 3.12 microg/mL. These compounds displayed better antifungal activity than that of standard oxiconazole. Furthermore, compound 22 carrying 4-chlorobenzylamino group at the 6-position of the purine moiety exhibited comparable antibacterial activity with that of the standard ciprofloxacin against both of the drug-resistant bacteria (MRSA, standard and clinical isolate).

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Tunçbilek M,Ateş-Alagöz Z,Altanlar N,Karayel A,Ozbey S

doi

10.1016/j.bmc.2008.12.050

subject

Has Abstract

pub_date

2009-02-15 00:00:00

pages

1693-700

issue

4

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)01231-5

journal_volume

17

pub_type

杂志文章

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