1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.
A range of novel 1,2,3-triazolylalkylribitol derivatives were synthesized and evaluated as nucleoside hydrolase inhibitors. The most active compound (11a) has low micromolar potency and is structurally diverse from previously reported nucleoside hydrolase inhibitors, which, along with the simplicity of the chemistry involved in its synthesis, makes it a good lead for the further development of novel nucleoside hydrolase inhibitors.
Goeminne
A
A
Department of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
McNaughton
M
M
Bal
G
G
Surpateanu
G
G
Van der Veken
P
P
De Prol
S
S
Versées
W
W
Steyaert
J
J
Apers
S
S
Haemers
A
A
Augustyns
K
K
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007700:Kinetics; D008956:Models, Chemical; D008968:Molecular Conformation; D009699:N-Glycosyl Hydrolases / Q000037:antagonists & inhibitors*; D012255:Ribitol / Q000031:analogs & derivatives* / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry*; D014346:Trypanosoma brucei brucei / Q000201:enzymology
D004791:Enzyme Inhibitors; D014230:Triazoles; D012255:Ribitol; D009699:N-Glycosyl Hydrolases