Probing stereoselective inhibition of the acyl binding site of cholesterol esterase with four diastereomers of 2'-N-α-methylbenzylcarbamyl-1, 1'-bi-2-naphthol

SY Chiou, CY Lai, LY Lin, G Lin - BMC biochemistry, 2005 - Springer
Background Recently there has been increased interest in pancreatic cholesterol esterase
due to correlation between enzymatic activity in vivo and absorption of dietary cholesterol …

Discovery of potential pancreatic cholesterol esterase inhibitors using pharmacophore modelling, virtual screening, and optimization studies

S John, S Thangapandian, S Sakkiah… - Journal of enzyme …, 2011 - Taylor & Francis
Pancreatic cholesterol esterase (CEase) is a serine hydrolase involved in the hydrolysis of
variety of lipids and transport of free cholesterol. In this study, pharmacophore hypotheses …

4-CF3-ezetimibe analogs: design, synthesis, and biological evaluation of cholesterol absorption inhibitions

Y Liu, JL Chen, GH Wang, P Sun, H Huang, FL Qing - Tetrahedron Letters, 2013 - Elsevier
On the purpose of looking for better cholesterol absorption inhibitors, several trifluoromethyl
substituted ezetimibe analogs 1a–d were designed and synthesized. The key steps in the …

Synthesis of tricyclic 1, 3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition

M Pietsch, M Gütschow - Journal of medicinal chemistry, 2005 - ACS Publications
A series of thieno [1, 3] oxazin-4-ones and thieno [1, 3] thiazin-4-ones were synthesized and
investigated as inhibitors of the α/β hydrolases cholesterol esterase (CEase) and …

Inhibition of porcine liver carboxylesterase by phosphorylated flavonoids

Y Wei, AY Peng, J Huang - Chemico-biological interactions, 2013 - Elsevier
We have recently synthesized a series of phosphorylated flavonoids and identified some of
them as potent inhibitors of pancreatic cholesterol esterase (CEase) with excellent selectivity …

Phosphaisocoumarins as a new class of potent inhibitors for pancreatic cholesterol esterase

B Li, B Zhou, H Lu, L Ma, AY Peng - European journal of medicinal …, 2010 - Elsevier
Due to the importance of pancreatic cholesterol esterase (CEase) as a potential target in
atherosclerosis and for the development of hypocholesterolemic agents, there are …

Alternate Substrate Inhibition of Cholesterol Esterase by Thieno [2, 3-d][1, 3] oxazin-4-ones* 210

M Pietsch, M Gütschow - Journal of Biological Chemistry, 2002 - ASBMB
In a kinetic study, the interaction of bovine pancreatic cholesterol esterase (CEase) with
fused 1, 3-oxazin-4-ones and 1, 3-thiazin-4-ones was investigated, and the compounds …

[HTML][HTML] Novel amino-β-lactam derivatives as potent cholesterol absorption inhibitors

T Dražić, K Molčanov, V Sachdev, M Malnar… - European journal of …, 2014 - Elsevier
Abstract Two new trans-(3R, 4R)-amino-β-lactam derivatives and their diastereoisomeric
mixtures were synthesized as ezetimibe bioisosteres and tested in in vitro and in vivo …

Total synthesis of ezetimibe, a cholesterol absorption inhibitor

M Sniezek, S Stecko, I Panfil, B Furman… - The Journal of …, 2013 - ACS Publications
Ezetimibe (1), a strong β-lactamic cholesterol absorption inhibitor, was synthesized from (R)-
6-(4-fluorophenyl)-5, 6-dihydro-2 H-pyran-2-one 7. Independent pathways were analyzed in …

[HTML][HTML] Inhibitory effect of procyanidin B2 and tannin acid on cholesterol esterase and their synergistic effect with orlistat

X Li, Y Pu, H Jiang, W Jiao, W Peng, W Tian… - Food Science and …, 2024 - Elsevier
This study was aimed to analyze the effect of procyanidin B 2 (PC) and tannin acid (TA) on
the activities of cholesterol esterase (CEase) and the inhibitory mechanisms of enzymatic …