Abstract

Several members of a new family of non-sugar-type α-glucosidase inhibitors, bearing a phthalimide moiety connected to a variously substituted phenoxy ring by an alkyl chain, were synthesized and their activities were investigated. The efficacy of the inhibition activity appeared to be governed by the chain length of the substrate. Substrates possessing 10 carbons afforded the highest levels of activity, which were one to two orders of magnitude more potent than the known inhibitor 1-deoxynojirimycin (dNM). Furthermore, structure-activity relationship studies indicated a critical role of electron-withdrawing substituents at the phenoxy group for the activity. Derivatives bearing a chlorine atom along with a strong electron-withdrawing group, such as a nitro group, were the most potent of the series.

Autore Pugliese

• Carocci Alessia , Catalano Alessia , De Palma Annalisa , Franchini Carlo , Lentini Giovanni , Cavalluzzi Maria Maddalena , Scalera Vito Dom. E.

Tutti gli autori

• CAROCCI A.;CATALANO A.;DE PALMA A.;FRANCHINI C.;LENTINI G.;CAVALLUZZI M.M.;SCALERA V.D.E.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2010

ISSN

0968-0896

ISBN

Non Disponibile

Numero di citazioni Wos

22

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

25

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile