Synthesis and biological evaluation of unprecedented classes of spiro-beta-lactams and azido-beta-lactams as acyl-CoA:cholesterol acyltransferase inhibitors.
Unprecedented classes of four- and five-membered hydroxyl-spiro-beta-lactams and hydroxyl-azido-beta-lactams were prepared via regioselective ring opening of hydroxyl-epoxides. The potential of these particular beta-lactams as biologically active compounds has been confirmed by the results obtained in ACAT inhibition assays.
Benfatti
Fides
F
Dipartimento di Chimica G. Ciamician, Università di Bologna, Via Selmi 2, 40126 Bologna, Italy.
Cardillo
Giuliana
G
Gentilucci
Luca
L
Tolomelli
Alessandra
A
D000042:Absorption; D000214:Acyl Coenzyme A / Q000737:chemistry; D002384:Catalysis; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002784:Cholesterol / Q000737:chemistry; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D004852:Epoxy Compounds / Q000737:chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D008968:Molecular Conformation; D002785:Sterol O-Acyltransferase / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D047090:beta-Lactams / Q000737:chemistry*
D000214:Acyl Coenzyme A; D004791:Enzyme Inhibitors; D004852:Epoxy Compounds; D047090:beta-Lactams; D002784:Cholesterol; D002785:Sterol O-Acyltransferase