Five-membered iminocyclitol α-glucosidase inhibitors: Synthetic, biological screening and in silico studies

…, R Moreira, AT Caldeira, RC Guedes, AJ Burke

Index: Guerreiro, Luis R.; Carreiro, Elisabete P.; Fernandes, Luis; Cardote, Teresa A.F.; Moreira, Rui; Caldeira, Ana T.; Guedes, Rita C.; Burke Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 7 p. 1911 - 1917

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Citation Number: 19

Abstract

The design and synthesis of a small library of pyrrolidine iminocyclitol inhibitors with a structural similarity to 1, 4-dideoxy-1, 4-imino-d-arabitol (DAB-1) is reported. This library was specifically designed to gain a better insight into the mechanism of inhibition of glycosidases by polyhydroxylated pyrrolidines or iminocyclitols. Pyrrolidine-3, 4-diol 15a and pyrrolidine- 3, 4-diol diacetate 15b had emerged as the most potent α-glucosidase inhibitors in the ...