title: Synthesis and biological evaluation of ureido and thioureido derivatives of 2-amino-2-deoxy-D-glucose and related aminoalcohols as N-acetyl-beta-D-hexosaminidase inhibitors.
abstract: Ureido and thioureido derivatives of 2-acetamido-2-deoxy-beta-D-glucose, 1-amino-1-deoxy-D-glucitol and 2-(2-aminoethoxy)ethanol were prepared as N-acetyl-beta-D-hexosaminidase (NAHase) inhibitors and were evaluated on Trichomonas vaginalis NAHase. Although none showed complete inhibition of the enzyme at 100 microM, 1-amino-1-deoxy-D-glucitol derivatives acted as competitive inhibitors of the NAHase of T. vaginalis.
authors.affiliation: Laboratoire de Chimie, Faculté de Pharmacie, Toulouse, France.
authors.forename: C
authors.initials: C
authors.lastname: Tournaire-Arellano
authors.forename: S Y
authors.initials: SY
authors.lastname: Hage
authors.forename: P
authors.initials: P
authors.lastname: Valès
authors.forename: R
authors.initials: R
authors.lastname: Caujolle
authors.forename: A
authors.initials: A
authors.lastname: Sanon
authors.forename: C
authors.initials: C
authors.lastname: Bories
authors.forename: P M
authors.initials: PM
authors.lastname: Loiseau
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis*; D000431:Ethanol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D005021:Ethylamines / Q000138:chemical synthesis*; D005069:Evaluation Studies as Topic; D005944:Glucosamine / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D015394:Molecular Structure; D013012:Sorbitol / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D014246:Trichomonas vaginalis / Q000201:enzymology; D001619:beta-N-Acetylhexosaminidases / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D005021:Ethylamines; D000431:Ethanol; D013012:Sorbitol; C119561:1-amino-1-deoxy-glucitol; C110684:2-(2-aminoethoxy)ethanol; D001619:beta-N-Acetylhexosaminidases; D005944:Glucosamine