Novel potent bifunctional carboxylesterase inhibitors based on a polyfluoroalkyl-2-imino-1, 3-dione scaffold

GF Makhaeva, SV Lushchekina, NP Boltneva… - European Journal of …, 2021 - Elsevier
An expanded series of alkyl 2-arylhydrazinylidene-3-oxo-3-polyfluoroalkylpropionates
(HOPs) 3 was obtained via Cu (OAc) 2-catalyzed azo coupling. All were nanomolar …

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 …

Recent progress in the discovery of natural inhibitors against human carboxylesterases

DD Wang, LW Zou, Q Jin, J Hou, GB Ge, L Yang - Fitoterapia, 2017 - Elsevier
Mammalian carboxylesterases (CEs) are important serine hydrolases catalyzing the
hydrolysis of ester-or amide-containing compounds into the corresponding alcohols and …

Synthesis, molecular docking, and biological evaluation of 3-oxo-2-tolylhydrazinylidene-4, 4, 4-trifluorobutanoates bearing higher and natural alcohol moieties as new …

GF Makhaeva, NA Elkina, EV Shchegolkov… - Bioorganic …, 2019 - Elsevier
To search for effective and selective inhibitors of carboxylesterase (CES), a series of 3-oxo-2-
tolylhydrazinylidene-4, 4, 4-trifluorobutanoates bearing higher or natural alcohol moieties …

Characterization and structure-activity relationship studies of flavonoids as inhibitors against human carboxylesterase 2

ZM Weng, GB Ge, TY Dou, P Wang, PK Liu, XH Tian… - Bioorganic …, 2018 - Elsevier
Human carboxylesterases (hCEs) are key enzymes from the serine hydrolase superfamily.
Among all identified hCEs, human carboxylesterase 2 (hCE2) plays crucial roles in the …

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 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 …

Discovery of natural pentacyclic triterpenoids as potent and selective inhibitors against human carboxylesterase 1

PF Song, YD Zhu, HY Ma, YN Wang, DD Wang… - Fitoterapia, 2019 - Elsevier
Abstract Human carboxylesterase 1 (CES1), primarily expressed in the liver and adipocytes,
is responsible for the hydrolysis of endogenous esters (such as cholesteryl esters and …

Synthesis of 2-arylhydrazinylidene-3-oxo-4, 4, 4-trifluorobutanoic acids as new selective carboxylesterase inhibitors and radical scavengers

OG Khudina, GF Makhaeva, NA Elkina… - Bioorganic & Medicinal …, 2019 - Elsevier
Abstract A series of 2-arylhydrazinylidene-3-oxo-4, 4, 4-trifluorobutanoic acids was
synthesized via dealkylation of ethyl 2-arylhydrazinylidene-3-oxo-4, 4, 4-trifluorobutanoates …

Rational approaches, design strategies, structure activity relationship and mechanistic insights for esterase inhibitors

H Singh, JV Singh, N Kaur, M Sanduja… - Mini Reviews in …, 2018 - ingentaconnect.com
Background: Esterase is an enzyme that splits esters into an acid and alcohol. Varieties of
esterases are present in human body to control diverse set of cellular processes and …