Structure-activity relationships of uridine 5'-diphosphate analogues at the human P2Y6 receptor.

The structure-activity relationships and molecular modeling of the uracil nucleotide activated P2Y6 receptor have been studied. Uridine 5'-diphosphate (UDP) analogues bearing substitutions of the ribose moiety, the uracil ring, and the diphosphate group were synthesized and assayed for activity at the human P2Y6 receptor. The uracil ring was modified at the 4 position, with the synthesis of 4-substituted-thiouridine 5'-diphosphate analogues, as well as at positions 2, 3, and 5.

Synthesis and study of conformationally restricted 3'-deoxy-3',4'-exo-methylene nucleoside analogues.

Hitherto unknown restricted 3'-deoxy-3',4'-exo-methylene nucleoside derivatives bearing the nucleic acid naturally occurring pyrimidine bases have been synthesized. The compounds were tested for their activity against HIV, HBV, and several RNA viruses, but they did not show significant antiviral effect.

Synthesis of nucleoside analogues bearing the five naturally occurring nucleic acid bases built on a 2-oxabicylo[3.1.0]hexane scaffold.

Hitherto unknown nucleoside analogues incorporating the five naturally occurring nucleic acid bases built on a 2-oxabicyclo[3.1.0]hexane template were synthesized.