α-Amino-α'-halomethylketones are interesting scaffolds bearing (at least) two sequential electrophilic carbons that by interacting with the nucleophilic moieties of several enzymes, represent the ideal candidates for in vivo and in vitro inhibition studies. In this work a summary of their use as optimal inhibitors of physiologically relevant serine and cysteine proteases is given with a particular emphasis on recently established SAR studies. A brief survey of the most relevant synthetic processes for their obtainment and the importance they possess in synthetic medicinal chemistry is reported.

α-amino-α'-halomethylketones : Synthetic methodologies and pharmaceutical applications as serine and cysteine protease inhibitors / V. Pace, L. Castoldi, M. Pregnolato. - In: MINI-REVIEWS IN MEDICINAL CHEMISTRY. - ISSN 1389-5575. - 13:7(2013 Jul 01), pp. 988-996. [10.2174/1389557511313070004]

α-amino-α'-halomethylketones : Synthetic methodologies and pharmaceutical applications as serine and cysteine protease inhibitors

L. Castoldi;
2013

Abstract

α-Amino-α'-halomethylketones are interesting scaffolds bearing (at least) two sequential electrophilic carbons that by interacting with the nucleophilic moieties of several enzymes, represent the ideal candidates for in vivo and in vitro inhibition studies. In this work a summary of their use as optimal inhibitors of physiologically relevant serine and cysteine proteases is given with a particular emphasis on recently established SAR studies. A brief survey of the most relevant synthetic processes for their obtainment and the importance they possess in synthetic medicinal chemistry is reported.
Aminoketones; Drug synthesis; Haloketones; Inhibitors; Proteases; Structure-activity relationship
Settore CHIM/06 - Chimica Organica
1-lug-2013
Article (author)
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/886964
Citazioni
  • ???jsp.display-item.citation.pmc??? 3
  • Scopus 13
  • ???jsp.display-item.citation.isi??? 14
social impact