Two conformationally constrained compounds similar to chicoric acid but lacking the catechol and carboxyl groups were prepared. In these analogues, the single bond between the two caffeoyl fragments has been replaced with a chiral oxirane ring and both aromatic residues modified protecting completely or partially the catechol moiety as methyl ether. Preliminary molecular modelling studies carried out on the two analogues showed interactions near the active site of HIV integrase; however, in comparison with raltegravir, the biological evaluation confirmed that CAA-1 and CAA-2 were unable to inhibit infection at lower concentration.
Righi, G., Pelagalli, R., Isoni, V., Tirotta, I., Dallocchio, R., Dessì, A., et al. (2017). Synthesis, molecular modeling and biological evaluation of two new chicoric acid analogs. NATURAL PRODUCT RESEARCH, 31(4), 397-403 [10.1080/14786419.2016.1169413].
Tipologia: | Articolo su rivista | |
Citazione: | Righi, G., Pelagalli, R., Isoni, V., Tirotta, I., Dallocchio, R., Dessì, A., et al. (2017). Synthesis, molecular modeling and biological evaluation of two new chicoric acid analogs. NATURAL PRODUCT RESEARCH, 31(4), 397-403 [10.1080/14786419.2016.1169413]. | |
URL: | www.tandf.co.uk/journals/titles/14786419.asp | |
IF: | Con Impact Factor ISI | |
Lingua: | English | |
Settore Scientifico Disciplinare: | Settore BIO/14 Settore CHIM/08 - Chimica Farmaceutica | |
Revisione (peer review): | Esperti anonimi | |
Tipo: | Articolo | |
Rilevanza: | Rilevanza internazionale | |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1080/14786419.2016.1169413 | |
Stato di pubblicazione: | Pubblicato | |
Data di pubblicazione: | feb-2017 | |
Titolo: | Synthesis, molecular modeling and biological evaluation of two new chicoric acid analogs | |
Autori: | ||
Autori: | Righi, G; Pelagalli, R; Isoni, V; Tirotta, I; Dallocchio, R; Dessì, A; Macchi, B; Frezza, C; Rossetti, I; Bovicelli, P | |
Appare nelle tipologie: | 01 - Articolo su rivista |
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