pyrazolo[4,3-e][1,2,4]triazines purine analogues with electronic absorption in the visible regionpyrazolo[4,3 e][1、2、4)三嗪嘌呤类似物的电子吸收可见区域.pdfVIP

Molecules 2005, 10, 1298-1306 molecules ISSN 1420-3049 Pyrazolo[4,3-e][1,2,4]triazines: Purine Analogues with Electronic Absorption in the Visible Region Mariusz Mojzych 1, Andrzej Rykowski 1,* and Jacek Wierzchowski 2 1 Department of Chemistry, University of Podlasie, 3-Maja 54, Siedlce, Poland, PL-08-110, Tel.+48- 6431090, Fax +48-6442045 2 Department of Biophysics, University of Warmia Mazury, 4 Oczapowskiego St., Olsztyn, Poland, PL-10-789, Tel. +48-89-523-3406, Fax +48 89 524-04-08, e-mail: jacek.wie@.pl * Author to whom correspondence should be addressed; e-mail: rykowski@ap.siedlce.pl Received: 12 April 2005 / Accepted: 10 July 2005 / Published: 31 October 2005 Abstract: Synthesis of several pryrazolo[4,3-e][1,2,4]-triazines is described. The absorption spectrum of some 5-substituted derivatives was found to extend to the visible region. These compounds were found to inhibit some enzymes of purine metabolism, like xanthine oxidase or bacterial purine-nucleoside phosphorylase with Ki values in the 10-3 – -5 10 M range. Keywords: Pyrazolo[4,3-e][1,2,4]triazines, purine analogues, enzyme inhibitors. Introduction Modified purine nucleosides and their analogues have found numerous applications in biological research and pharmacology [1-3]. In particular, the isomeric pyrazolopyrimidines and triazolopyrimidines (8-azapurines) exhibit favourable spectroscopic and biochemical properties and have potential for use in cancer and viral chemotherapy [3-6]. It has been found recently that another class of naturally occurrin