A series of N-(2,4-difluorophenyl)-N′-heptyl-N′-{4- [(substituted)-pyridazin-3-yl)thio]pentyl}urea derivatives having a phenyl ring at positions 5 and/or at position 6 of the heterocycle, as well as the corresponding sulfones, were synthesized. Their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. Theoretical studies were performed to correlate their activity to their structural features.
Ureidopyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors / A. Gelain, I. Bettinelli, D. Barlocco, B-M. Kwon, T-S. Jeong, K-R. Im, L. Legnani, L. Toma. - In: SCIENTIA PHARMACEUTICA. - ISSN 0036-8709. - 74:3(2006), pp. 85-97.
Ureidopyridazine derivatives as acyl-CoA:cholesterol acyltransferase inhibitors
A. GelainPrimo
;D. Barlocco;
2006
Abstract
A series of N-(2,4-difluorophenyl)-N′-heptyl-N′-{4- [(substituted)-pyridazin-3-yl)thio]pentyl}urea derivatives having a phenyl ring at positions 5 and/or at position 6 of the heterocycle, as well as the corresponding sulfones, were synthesized. Their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. Theoretical studies were performed to correlate their activity to their structural features.
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
