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1 article(s) from Parenti, Paolo

Synthesis and biological evaluation of nojirimycin- and pyrrolidine-based trehalase inhibitors

Davide Bini,
Francesca Cardona,
Matilde Forcella,
Camilla Parmeggiani,
Paolo Parenti,
Francesco Nicotra and
Laura Cipolla

Beilstein J. Org. Chem. 2012, 8, 514–521, doi:10.3762/bjoc.8.58

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Graphical Abstract

Figure 1: Structure of trehalose (1), validoxylamine A (2), 1-thiatrehazolin (3), trehalostatin (4), casuarin...

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Figure 2: Structure of nojirimycin-based (7, 8) and pyrrolidine-based (9) leads.

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Figure 3: Structures of potential inhibitors 10–21.

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Scheme 1: Synthesis of nojirimycin-based inhibitors 10,12 and 13. Reagents and conditions: (a) H₂, Pd/C, NH₄O...

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Scheme 2: Synthesis of pyrrolidine derivatives 14, 16, 17 and 19. Reagents and conditions: (a) H₂, Pd(OH)₂/C,...

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Scheme 3: Synthesis of pyrrolidines 20 and 21. Reagents and conditions: (a) H₂, Pd/C, MeOH, HCl; (b) octanal,...

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Figure 4: Histogram of the inhibitory activity of compounds 7–10, 12–14, 16 and 20. Derivatives 10, 14 and 16...

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Published 05 Apr 2012

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