New cholesterol esterase inhibitors based on rhodanine and thiazolidinedione scaffolds

S Heng, W Tieu, S Hautmann, K Kuan… - Bioorganic & medicinal …, 2011 - Elsevier
We present a new class of inhibitors of pancreatic cholesterol esterase (CEase) based on
'priviledged'5-benzylidenerhodanine and 5-benzylidene-2, 4-thiazolidinedione structural …

[HTML][HTML] 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 …

Isocoumarin-based inhibitors of pancreatic cholesterol esterase

JJ Heynekamp, LA Hunsaker, TA Vander Jagt… - Bioorganic & medicinal …, 2008 - Elsevier
Pancreatic cholesterol esterase (CEase), which is secreted from the exocrine pancreas, is a
serine hydrolase that aids in the bile salt-dependent hydrolysis of dietary cholesteryl esters …

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 …

Benzoflavones as cholesterol esterase inhibitors: Synthesis, biological evaluation and docking studies

H Singh, JV Singh, MK Gupta, P Singh… - Bioorganic & Medicinal …, 2017 - Elsevier
Abstract A library of forty 7, 8-benzoflavone derivatives was synthesized and evaluated for
their inhibitory potential against cholesterol esterase (CEase). Among all the synthesized …

A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors

G Peng, Y Du, Y Wei, J Tang, AY Peng… - Organic & Biomolecular …, 2011 - pubs.rsc.org
Five flavones possessing one to four phenolic groups were fully phosphorylated efficiently
and the obtained compounds showed excellent pancreatic cholesterol esterase (CEase) …

Identification and synthesis of selective cholesterol esterase inhibitor using dynamic combinatorial chemistry

S Zhao, Y Wu, L Hu - Bioorganic Chemistry, 2022 - Elsevier
In this study, the concept of dynamic combinatorial chemistry (DCC) was applied to explore
novel cholesterol esterase (CEase) inhibitors. In the presence of enzyme, two substrates …

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 …

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 …

Potential human cholesterol esterase inhibitor design: benefits from the molecular dynamics simulations and pharmacophore modeling studies

S John, S Thangapandian, KW Lee - Journal of Biomolecular …, 2012 - Taylor & Francis
Human pancreatic cholesterol esterase (hCEase) is one of the lipases found to involve in
the digestion of large and broad spectrum of substrates including triglycerides …