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