Synthesis of new carboxylesterase inhibitors and evaluation of potency and water solubility

CE Wheelock, TF Severson… - Chemical research in …, 2001 - ACS Publications
Carboxylesterases are essential enzymes in the hydrolysis and detoxification of numerous
pharmaceuticals and pesticides. They are vital in mediating organophosphate toxicity and in …

Substituted trifluoroketones as potent, selective inhibitors of mammalian carboxylesterases

MBA Ashour, BD Hammock - Biochemical pharmacology, 1987 - Elsevier
A series of substituted trifluoroketones were tested as inhibitors of mammalian liver
microsomal carboxylesterase (s) hydrolyzing a variety of substrates including malathion …

Identification and characterization of novel benzil (diphenylethane-1, 2-dione) analogues as inhibitors of mammalian carboxylesterases

RM Wadkins, JL Hyatt, X Wei, KJP Yoon… - Journal of medicinal …, 2005 - ACS Publications
Carboxylesterases (CE) are ubiquitous enzymes responsible for the metabolism of
xenobiotics. Because the structural and amino acid homology among esterases of different …

Structure-activity relationships for substrates and inhibitors of mammalian liver microsomal carboxylesterases

TL Huang, T Shiotsuki, T Uematsu, B Borhan… - Pharmaceutical …, 1996 - Springer
Purpose. Carboxylesterases are important in the detoxification of drugs, pesticides and other
xenobiotics. This study was to evaluate a series of substrates and inhibitors for …

Use of ab initio calculations to predict the biological potency of carboxylesterase inhibitors

CE Wheelock, ME Colvin, I Uemura… - Journal of medicinal …, 2002 - ACS Publications
Carboxylesterases are important enzymes responsible for the hydrolysis and metabolism of
numerous pharmaceuticals and xenobiotics. These enzymes are potently inhibited by …

Carboxylesterases—from function to the field: an overview of carboxylesterase biochemistry, structure–activity relationship, and use in environmental field monitoring

CE Wheelock, Y Nakagawa - Journal of Pesticide Science, 2010 - jstage.jst.go.jp
Special Topic (hiCE, CES2A1) involved in the activation of CPT-11 in the intestine, but do
not affect hCE1 activity. They then discuss several strategies for in silico drug development …

Carboxylesterase inhibitors: an update

LW Zou, Q Jin, DD Wang, QK Qian… - Current medicinal …, 2018 - ingentaconnect.com
Mammalian carboxylesterases are key serine hydrolases that catalyze the hydrolysis of a
wide variety of ester compounds in the corresponding carboxylic acids and alcohols. In …

Carboxylesterase inhibitors

MJ Hatfield, PM Potter - Expert opinion on therapeutic patents, 2011 - Taylor & Francis
Introduction: Carboxylesterases play major roles in the hydrolysis of numerous
therapeutically active compounds. This is, in part, due to the prevalence of the ester moiety …

Requirements for mammalian carboxylesterase inhibition by substituted ethane-1, 2-diones

EI Parkinson, MJ Hatfield, L Tsurkan, JL Hyatt… - Bioorganic & medicinal …, 2011 - Elsevier
Carboxylesterases (CE) are ubiquitous enzymes found in both human and animal tissues
and are responsible for the metabolism of xenobiotics. This includes numerous natural …

Structure− Activity Relationships of Substituted 1-Pyridyl-2-phenyl-1, 2-ethanediones: Potent, Selective Carboxylesterase Inhibitors

BM Young, JL Hyatt, DC Bouck, T Chen… - Journal of medicinal …, 2010 - ACS Publications
Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/
pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously …