Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5 ' and 8

Authors
Aronov, AM Gelb, MH
Citation
Am. Aronov et Mh. Gelb, Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5 ' and 8, BIOORG MED, 8(24), 1998, pp. 3505-3510
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
24
Year of publication
1998
Pages
3505 - 3510
Database
ISI
SICI code
0960-894X(199812)8:24<3505:SASROA>2.0.ZU;2-U
Abstract
A number of 5', N-6- and C-8, N-6-disubstituted adenosine analogs was synth esized and tested for inhibition of trypanosomal glyceraldehyde 3-phosphate dehydrogenase. The most active compound, N-6-(3-methyl-2-butenyl)-8-(2-thi enyl)adenosine had K-l of 9 mu M and was marginally selective for the paras ite enzyme. (C) 1998 Elsevier Science Ltd. All rights reserved.