Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5′ and 8
a Department of Chemistry, University of Washington, Seattle, WA 98195, U.S.A.
b Department of Biochemistry, University of Washington, Seattle, WE 98195, U.S.A.
Abstract:
A number of 5′, N6- and C8, N6-disubstituted adenosine analogs was synthesized and tested for inhibition of trypanosomal glyceraldehyde 3-phosphate dehydrogenase. The most active compound, N6-(3-methyl-2-butenyl)-8-(2-thienyl)adenosine, had Ki of 9 μM and was marginally selective for the parasite enzyme.