Synthesis of branched 9-[2-(2-phosphonoethoxy)ethyl]purines as a new class of acyclic nucleoside phosphonates which inhibit Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase

0329066 - ÚOCHB 2010 RIV GB eng J - Journal Article
Hocková, Dana - Holý, Antonín - Masojídková, Milena - Keough, D. T. - de Jersey, J. - Guddat, L. W.
Synthesis of branched 9-[2-(2-phosphonoethoxy)ethyl]purines as a new class of acyclic nucleoside phosphonates which inhibit Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase.
Bioorganic & Medicinal Chemistry. Roč. 17, č. 17 (2009), s. 6218-6232. ISSN 0968-0896. E-ISSN 1464-3391
R&D Projects: GA MŠMT 1M0508; GA AV ČR 1QS400550501
Institutional research plan: CEZ:AV0Z40550506
Keywords : acyclic nucleoside phosphonates * drug design * phosphoribosyltransferase * enzyme inhibitors * purine salvage pathway
Subject RIV: CC - Organic Chemistry
Impact factor: 2.822, year: 2009

Hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT) is the key enzyme in purine metabolism of the malarial parasite Plasmodium falciparum (Pf). Two series of novel branched ANPs derived from 9-[2-(2-phosphonoethoxy)ethyl]purines were synthesized to investigate their inhibition of Pf and human 6-oxopurine phosphoribosyltransferase.
Permanent Link: http://hdl.handle.net/11104/0175201