Ama-isomeric bicyclo[4.1.0]heptane analogues amabili e-glycosidase inhibitor galacto-validamine, (1R*,2S,3S,4S,5S,6S*) -5-amino-1-(hydroxymethyl)bicyclo[4.1.0]heptane -2,3,4-triol, iye yahlanganiswa ngezinyathelo ezingu-13 ukusuka ku-2,3,4,6-tetra-O-benzyl-D-galactose.Imisebenzi evimbelayo yama-amine amabili akhawulelwe ngokuvumelana, kanye nama-acetamide ahambisanayo, kukalwa ngama-enzyme entengiso e-alpha-galactosidase avela kubhontshisi wekhofi kanye ne-E. coli.Umsebenzi womndeni we-glycosyl hydrolase i-enzyme ye-GH27 (ubhontshisi wekhofi) uvinjwe ngokuncintisana i-1R,6S-amine (7), ukusebenzelana okubophayo okuphawulwe ivelu ye-K(i) engu-0.541 microM.I-GH36 E. coli alpha-galactosidase ibonise ukusebenzisana okubophezelayo okubuthakathaka kakhulu ne-1R,6S-amine (IC(50)= 80 microM).I-diastereomeric 1S,6R-amine (9) iboshelwe ngokubuthakathaka kuzo zombili i-galactosidase, (ubhontshisi wekhofi, IC(50)= 286 microM) kanye (E. coli, IC(50)= 2.46 mM).
