title: Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors.
abstract: A collection of (2R,3R,4S)-3,4-dihydroxypyrrolidin-2-yl derivatives have been tested for their inhibitory activities toward 25 glycosidases. Competitive (K(i)=7.4 microM) and selective inhibition of alpha-mannosidase from jack bean has been found for (2R,3R,4S)-2-[(benzylamino)methyl]pyrrolidine-3,4-diol and other derivatives.
authors.affiliation: Section de Chimie de l'Université de Lausanne, BCH, CH-1015 Lausanne-Dorigny, Switzerland.
authors.forename: F
authors.initials: F
authors.lastname: Popowycz
authors.forename: S
authors.initials: S
authors.lastname: Gerber-Lemaire
authors.forename: R
authors.initials: R
authors.lastname: Demange
authors.forename: E
authors.initials: E
authors.lastname: Rodriguez-García
authors.forename: A T
authors.initials: AT
authors.lastname: Asenjo
authors.forename: I
authors.initials: I
authors.lastname: Robina
authors.forename: P
authors.initials: P
authors.lastname: Vogel
mesh_terms: D000818:Animals; D002417:Cattle; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008361:Mannosidases / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D043323:alpha-Mannosidase
chemical_list: D004791:Enzyme Inhibitors; D008361:Mannosidases; D043323:alpha-Mannosidase