Small-molecule peptidomimetic inhibitors that already showed activity towards Secreted aspartic protease 2 as anti-Candida agents are herein presented as candidate HIV protease inhibitors. A library of 6,8-dioxa-3-azabicyclo[3.2.1]-octane peptidomimetic scaffolds was screened towards HIV protease, resulting in the identification of hit compounds possessing IC50 in the sub-micromolar range, and showing the bicyclic acetal portion as a potential transition state analogue in the interaction with catalytic aspartic acid residues.

Identification of constrained peptidomimetic chemotypes as HIV protease inhibitors / Chiara Calugi; Antonio Guarna; Andrea Trabocchi. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 84:(2014), pp. 444-453. [10.1016/j.ejmech.2014.07.049]

Identification of constrained peptidomimetic chemotypes as HIV protease inhibitors

CALUGI, CHIARA;GUARNA, ANTONIO;TRABOCCHI, ANDREA
2014

Abstract

Small-molecule peptidomimetic inhibitors that already showed activity towards Secreted aspartic protease 2 as anti-Candida agents are herein presented as candidate HIV protease inhibitors. A library of 6,8-dioxa-3-azabicyclo[3.2.1]-octane peptidomimetic scaffolds was screened towards HIV protease, resulting in the identification of hit compounds possessing IC50 in the sub-micromolar range, and showing the bicyclic acetal portion as a potential transition state analogue in the interaction with catalytic aspartic acid residues.
2014
84
444
453
Chiara Calugi; Antonio Guarna; Andrea Trabocchi
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/882121
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