Mono- and diphenylpyridazine ureido derivs. I (R1 = Ph, R2 = Ph; R1 = H, R2 = Ph; R1 = Ph, R2 = H; X = S, SO, SO2, or NH), structurally related to DuP 128 (II), were synthesized and tested for their inhibitory activity against ACAT isolated from rat liver microsomes. Several compds. displayed ACAT inhibition in the micromolar range. The amino derivs. I (R1 = Ph, R2 = Ph; R1 = H, R2 = Ph; R1 = Ph, R2 = H; X = NH) were also tested against hACAT-1 and hACAT-2 isoforms. They retained the same trend shown in the previous assay. Modeling studies on representative terms were performed. Significant similarities between the geometrical features of the model DuP 128 and the most active pyridazine derivs. were obsd.
Mono- or Diphenylpyridazines Connected to N-(2,4-Difluorophenyl)-N'-heptylurea as Acyl-CoA:Cholesterol Acyltransferase Inhibitors / A. Gelain, I. Bettinelli, D. Barlocco, B.M. Kwon, T.S. Jeong, K.H. Cho, L. Toma. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 48:24(2005), pp. 7708-7713. [10.1021/jm050703x]
Mono- or Diphenylpyridazines Connected to N-(2,4-Difluorophenyl)-N'-heptylurea as Acyl-CoA:Cholesterol Acyltransferase Inhibitors
A. GelainPrimo
;D. Barlocco;
2005
Abstract
Mono- and diphenylpyridazine ureido derivs. I (R1 = Ph, R2 = Ph; R1 = H, R2 = Ph; R1 = Ph, R2 = H; X = S, SO, SO2, or NH), structurally related to DuP 128 (II), were synthesized and tested for their inhibitory activity against ACAT isolated from rat liver microsomes. Several compds. displayed ACAT inhibition in the micromolar range. The amino derivs. I (R1 = Ph, R2 = Ph; R1 = H, R2 = Ph; R1 = Ph, R2 = H; X = NH) were also tested against hACAT-1 and hACAT-2 isoforms. They retained the same trend shown in the previous assay. Modeling studies on representative terms were performed. Significant similarities between the geometrical features of the model DuP 128 and the most active pyridazine derivs. were obsd.Pubblicazioni consigliate
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