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Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-beta-D-glucopyranosylamines
(2014)
Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-beta-D-glucopyranosylamines ...
Triazole pyrimidine nucleosides as inhibitors of Ribonuclease A. Synthesis, biochemical, and structural evaluation
(2012)
Five ribofuranosyl pyrimidine nucleosides and their corresponding 1,2,3-triazole derivatives have been synthesized and characterized. Their inhibitory action to Ribonuclease A has been studied by biochemical analysis and ...
STEREOCONTROLLED FACILE SYNTHESIS AND BIOLOGICAL EVALUATION OF (3 ' S) AND (3 ' R)-3 '-AMINO (AND AZIDO)-3 '-DEOXY PYRANONUCLEOSIDES
(2012)
This article describes the synthesis of (3'S) and (3'R)-3'-amino-3'-deoxy pyranonucleosides and their precursors (3'S) and (3'R)-3'-azido-3'-deoxy pyranonucleosides. Azidation of 1,2:5,6-di-O-isopropylidene-3-O-toluenesu ...
Branched-chain sugar nucleosides: stereocontrolled synthesis and bioevaluation of novel 3 '-C-trifluoromethyl and 3 '-C-methyl pyranonucleosides
(2015)
A new series of 3 '-C-trifluoromethyl- and 3 '-C-methyl-beta-D-allopyranonucleosides of 5-fluorouracil and their deoxy derivatives has been designed and synthesized. Treatment of ketosugar 1 with trifluoromethyltrimethylsilane ...
Stereocontrolled synthesis of 4 '-C-cyano and 4 '-C-cyano-4 '-deoxy pyrimidine pyranonucleosides as potential chemotherapeutic agents
(2012)
A new series of 4'-C-cyano and 4'-C-cyano-4'-deoxy pyrimidine pyranonucleosides has been designed and synthesized. Commercially available 1,2,3,4,6-penta-O-acetyl-D-mannopyranose (1) was condensed with silylated 5-fluorouracil, ...
Stereoselective facile synthesis of 2 '-spiro pyrimidine pyranonucleosides via their key intermediate 2 '-C-cyano analogues. Evaluation of their bioactivity
(2014)
A novel series of 2'-spiro pyrimidine pyranonucleosides has been designed and synthesized. Their precursors, 2'-C-cyano nucleosides 5a,b and 6a,b, were obtained by subjecting 1a,b to the sequence of selective protection ...
Synthesis of Novel Thiopurine Pyranonucleosides: Evaluation of Their Bioactivity
(2015)
We report the synthesis of novel thiopurine pyranonucleosides. Direct coupling of silylated 6-mercaptopurine and 6-thioguanine with the appropriate pyranoses 1a-e via Vorbruggen nucleosidation, gave the N-9 linked ...