Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1

J Zhang, QS Pan, XK Qian, XL Zhou… - Journal of Enzyme …, 2022 - Taylor & Francis
Pancreatic lipase (PL) is a well-known key target for the prevention and treatment of obesity.
Human carboxylesterase 1A (hCES1A) has become an important target for the treatment of …

(−)-SCH 57939: synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor

MP Kirkup, R Rizvi, BB Shankar, S Dugar… - Bioorganic & Medicinal …, 1996 - Elsevier
Previous SAR studies of C-3 side chain modified analogs of (−)-SCH 48461, 1, 3, 4 as well
as information concerning the metabolic stability this series, enabled us to design a …

Discovery, synthesis and evaluation of novel cholesterol absorption inhibitors

X Zhu, J Ji, D Huang, Y Zhu, C Tang… - Chemical Biology & …, 2012 - Wiley Online Library
Chemical‐based common feature pharmacophore modelling of Niemann Pick C1 Like 1
inhibitors was performed to provide some insights on the important pharmacophore features …

Structure related inhibition of enzyme systems in cholinesterases and BACE1 in vitro by naturally occurring naphthopyrone and its glycosides isolated from Cassia …

S Shrestha, SH Seong, P Paudel, HA Jung, JS Choi - Molecules, 2017 - mdpi.com
Cassia obtusifolia Linn. have been used to improve vision, inflammatory diseases, and as
hepatoprotective agents and to promote urination from ancient times. In the present study …

Carboxy-substituted 2-azetidinones as cholesterol absorption inhibitors

WD Vaccaro, R Sher, HR Davis Jr - Bioorganic & medicinal chemistry …, 1998 - Elsevier
Metabolism initiated SAR studies led to the discovery of a new class of potent 2-azetidinone
cholesterol absorption inhibitors. These studies found that a heteroatom at the para position …

Ezetimibe analogs with a reorganized azetidinone ring: Design, synthesis, and evaluation of cholesterol absorption inhibitions

X Xu, R Fu, J Chen, S Chen, X Bai - Bioorganic & Medicinal Chemistry …, 2007 - Elsevier
The underlying principle of drug design in this paper is that the maximum retention of the
functional groups that exist in the marketed drug would provide a higher probability for …

β-Lactam cholesterol absorption inhibitors

DA Burnett - Current medicinal chemistry, 2004 - ingentaconnect.com
β-Lactams have recently been identified as potent, highly efficacious cholesterol absorption
inhibitors (CAIs). The discovery, SAR, and asymmetric synthesis of this class of …

2-Azetidinone derivatives: Design, synthesis and evaluation of cholesterol absorption inhibitors

Y Wang, H Zhang, W Huang, J Kong, J Zhou… - European journal of …, 2009 - Elsevier
Fourteen new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been
synthesized, and three of them were enantiomerically pure. All the new compounds were …

Inhibitors of acyl-CoA: cholesterol acyltransferase: novel trisubstituted ureas as hypocholesterolemic agents

TS Purchase, AD Essenburg, KL Hamelehle… - Bioorganic & medicinal …, 1997 - Elsevier
Our continued interest in developing novel, potent acyl-CoA: cholesterol acyltransferase
(ACAT) inhibitors, and our discovery of several active series of disubstituted urea ACAT …

Novel protostane-type triterpenoids with inhibitory human carboxylesterase 2 activities

ZJ Zhang, XK Huo, XG Tian, L Feng, J Ning, XY Zhao… - RSC …, 2017 - pubs.rsc.org
The rhizomes of Alisma orientalis have been used for centuries in China and other Asian
countries as an effective herbal remedy. The phytochemical investigation of A. orientalis and …