Yeast a-glucosidase inhibitor

Bacillus cereus, against, 64 bacterial infections, 240 bacterial lipopolysaccharides, 1 Baker s yeast a-glucosidase inhibitor, 11 biochemistry and pathology in big, 320 biological, 1,75, 105, 193, 209, 212,... 

An analogous mechanism that relies on proton transfer and nucleophilic attack is apparently operative with aziridine derivatives of conduritol and deoxynojirimycin. Preliminary studies show both compounds are effective inhibitors the conduritol B aziridine (X) irreversibly inactivates Alcaligenesfaecalis )3-glucosidase and yeast a-glucosidase (2i8),and the ga/ac/odeoxynojirimycin aziridine (XI)... 

Dideoxy-1,4-imino-D-arabiiutol 2R, >RAR)-2-hydroxymethyl pyrrolidine-3,4-diol, DABl, 1] has been found in ho h Arachniodes standishii andAngylocalyx boutiqueanus and it is a potent inhibitor of yeast a-glucosidase (50% inhibition at 1.8 x 10 ... 

A multi-step synthesis of ot-fucosidase inhibitor 255 (Ki=6.4 pM) from 254 was reported (Scheme 18). Neither yeast a-glucosidase or E.coli P-galactosidase are inhibited by 255 at concentrations <1 mM (See also ChapterlS). ... 

The a-5-C-(l,3-dihydroxybutyl) derivative of hyacinthacine Ai 18 was reported to be a good inhibitor of yeast a-glucosidase and bacterial p-glucosi-dase, whereas 19 with the additional OH on the side chain, is a weaker inhibitor of the both enzymes. Alkaloid 25, regarded as a 5-C-(3-hydroxybutyl) derivative of A2, exhibits no activity, indicating that this long side chain plays an important role in the inhibition of the compounds (Table 1). 

Standard methods have been employed to prepare iV-acetyl-9-thio- and iV-acetyl-9-5-acetyl-9-thio-neuraminic acid and their methyl o-glycosides. Sulfoqui-novosyl diacylglycerols 9, isolated from the edible brown alga HizUcia fusiforme, are inhibitors of yeast a-glucosidase. ... 

Not unexpectedly by comparison with the monofluorinated 1-deoxynojirimycin derivatives, the 4,4-difluoro derivative 102 (Scheme 26) was found to be inactive with almond (l-glucosidase and the a-glucosidase from yeast.227 Equally inactive with these enzymes was the 3,3-difluoro compound 105 (Scheme 26).228 It is noteworthy that the 4,4-difluoro derivative of 1-deoxymannojirimycin, 103 (pAfa 5.3) turned out a good inhibitor of the (1-glucosidase from almonds (K, 45 pM, at pH 6.8 2 47 pM) and remained unprotonated and active at pH 5 (K, 92 pM 2 Kt 300 pM)227... 

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