Mechanistic studies of the inactivation of TEM-1 and P99 by NXL104, a novel non-β-lactam β-lactamase inhibitor

T Stachyra, MC Péchereau, JM Bruneau… - Antimicrobial agents …, 2010 - Am Soc Microbiol
ABSTRACT NXL104 is a potent inhibitor of class A and C serine β-lactamases, including
KPC carbapenemases. Native and NXL104-inhibited TEM-1 and P99 β-lactamases …

Synthesis and biological evaluation of phosphorylated flavonoids as potent and selective inhibitors of cholesterol esterase

Y Wei, AY Peng, B Wang, L Ma, G Peng, Y Du… - European Journal of …, 2014 - Elsevier
A series of phosphorylated flavonoids were synthesized and investigated in vitro as
inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE). The …

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 …

Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase

GC Muscia, S Hautmann, GY Buldain, SE Asís… - Bioorganic & Medicinal …, 2014 - Elsevier
Abstract A series of 2-(substituted) phenyl and 2-indolyl quinoline derivatives (10a–l) was
synthesized by an efficient microwave-assisted, trifluoroacetic acid-catalyzed, solvent-free …

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 …

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) …

One-pot synthesis of cinnamylamines with various protecting groups from cinnamyl ethers

YH Jung, JD Kim - Archives of pharmacal research, 2001 - Springer
The reaction of various alkyl cinnamyl ethers with CSI afforded the corresponding
cinnamylamines with various protecting groups, such as-NHMoc,-NHiPoc,-NHCbz,-NHPnz …

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 …

A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1, n-alkane-di-N-butylcarbamates

G Lin, HC Tseng, AC Chio, TM Tseng… - Bioorganic & medicinal …, 2005 - Elsevier
Alkane-1-N-butylcarbamate-n-ols (1–7) and 1, n-alkane-di-N-butylcarbamates (8–14) are
potent pseudo-substrate inhibitors of acetylcholinesterase. For inhibitors 1–7, the pre-steady …

Quantitative structure‐activity relationships for the pre‐steady state acetylcholinesterase inhibition by carbamates

G Lin, WC Liao, CH Chan, YH Wu… - … of Biochemical and …, 2005 - Wiley Online Library
Nitrophenyl-N-substituted carbamates (1) are characterized as pseudosubstrate inhibitors of
acetylcholinesterase. The first step is formation of the enzyme-inhibitor tetrahedral …