Synthesis and biological evaluation of novel heterocyclic ionone-like derivatives as anti-inflammatory agents.
Five- and six-membered heterocyclic ionone-like derivatives 4-6 have been synthesised in one step and with good yield from the key intermediate 3a and appropriate bifunctional reagents. Four were active as inhibitors of the respiratory burst of human neutrophils without affecting cell viability. The two most active compounds (5a,d) tested in neutrophil migration assays, were also found to be potent inhibitors of neutrophil chemotactic responsiveness. These two molecules could be considered as lead compounds of new drugs which can be an effective tool to treat psoriasis and related neutrophilic dermatoses.
Balbi
Alessandro
A
Dipartimento di Scienze Farmaceutiche, Viale Benedetto XV, 3 Genova, Italy. balbi@unige.it
Anzaldi
Maria
M
Mazzei
Mauro
M
Miele
Mariangela
M
Bertolotto
Maria
M
Ottonello
Luciano
L
Dallegri
Franco
F