Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors.
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.
Popowycz
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F
Section de Chimie de l'Université de Lausanne, BCH, CH-1015 Lausanne-Dorigny, Switzerland.
Gerber-Lemaire
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Demange
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Rodriguez-García
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E
Asenjo
A T
AT
Robina
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Vogel
P
P
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
D004791:Enzyme Inhibitors; D008361:Mannosidases; D043323:alpha-Mannosidase