Article

 

Synthesis and Biological Activity of Novel 6–Substituted Purine Derivatives

 

Yu Lin Hu, Xiang Liu, and Ming Lu^*

 

Chemical Engineering College, Nanjing University of Science and Technology, Nanjing 210094, PR China, Tel: 86–02584315030, Fax: 86–025–84315030, ^*Responsible author: luming1963@163.com

 

Received December 9, 2009
Accepted March 5, 2010

 

Abstract

A series of 6–substituted purines were synthesized from commercially available 2–amino–6–chloropurine with appropriate reagents, and nine new compounds 7, 8, and 11–17 have been discovered. The compounds synthesized were identified by elemental analysis, ¹H NMR, as well as mass spectral data. All the title compounds were screened for their antifungal activities, under the method of the disc diffusion, using three species of fungi — Bacillus subtillis, Aspergillus niger, and Candida tropicalis— and some of the compounds showed promising activities.

Key words: 6–Substituted purines, 2–amino–6–chloropurine, Synthesis, Antifungal Activity.

 

Resumen

Se preparó una serie de purinas 6–sustituidas a partir de la 2–amino–6–cloropurina, que está disponible comercialmente, y de los reactivos apropiados, de los cuales los derivados 7, 8 y 11–17 no han sido reportados previamente. Los compuestos sintetizados se caracterizaron por análisis elemental, RMN ¹H y espectrometría de masas. Todos los compuestos se evaluaron en su actividad antifúngica, a través del método de difusión de discos, sobre tres especies de hongos — Bacillus subtillis, Aspergillus niger y Candida tropicalis—, mostrando algunos de ellos una actividad promisoria.

Palabras clave: Purinas 6–sustituidas, 2–amino–6–cloropurina, síntesis, actividad antifúngica.

 

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Acknowledgement

We thank the National Basic Research Program (973 Program) of China and Ministry of Education of the Republic of China for support of this research.

 

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