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Design, synthesis, and pharmacological characterization of novel spirocyclic quinuclidinyl-Δ2-isoxazoline derivatives as potent and selective agonists of α7 nicotinic acetylcholine receptors.Drug discovery targeting amino acid racemases.A novel spirocyclic tropanyl-Δ²-isoxazoline derivative enhances citalopram and paroxetine binding to serotonin transporters as well as serotonin uptake.Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria.Mechanism of inhibition of the glutamate transporter EAAC1 by the conformationally constrained glutamate analogue (+)-HIP-BSynthesis and in vitro/in vivo evaluation of the antitrypanosomal activity of 3-bromoacivicin, a potent CTP synthetase inhibitor.Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antiprotozoal agents.New spirocyclic Δ²-isoxazoline derivatives related to selective agonists of α7 neuronal nicotinic acetylcholine receptors.Neuroprotective effects of the novel glutamate transporter inhibitor (-)-3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]-isoxazole-4-carboxylic acid, which preferentially inhibits reverse transport (glutamate release) compared with glutamate reuptaSynthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.Synthesis and biological evaluation of CTP synthetase inhibitors as potential agents for the treatment of African trypanosomiasis.Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: design, synthesis, and pharmacological characterization.Design and synthesis of novel isoxazole-based HDAC inhibitors.Novel potent AMPA/kainate receptor antagonists: synthesis and anticonvulsant activity of a series of 2-[(4-alkylsemicarbazono)-(4-amino-phenyl)methyl]-4,5-methylenedioxyphenylacetic acid alkyl esters.Synthesis and pharmacology of 3-hydroxy-delta2-isoxazoline-cyclopentane analogues of glutamic acid.Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists.Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids.Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands.Design of 1-substituted 2-arylmethyl-4,5-methylenedioxybenzene derivatives as antiseizure agents.Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists.Investigating the mechanism of substrate uptake and release in the glutamate transporter homologue Glt(Ph) through metadynamics simulations.Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.Synthesis and pharmacological characterization of new chiral derivatives of muscarine and allo-muscarine.Alpha7 nicotinic acetylcholine receptor agonists: prediction of their binding affinity through a molecular mechanics Poisson-Boltzmann surface area approach.Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead.Synthesis of novel pyrrolo[3,4-d]pyrazole-dicarboxylic acids and evaluation of their interaction with glutamate receptors.Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit.Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids.New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists.Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M.New analogues of oxotremorine and oxotremorine-M: estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes.Synthesis of enantiopure Delta2-isoxazoline derivatives and evaluation of their affinity and efficacy profiles at human beta-adrenergic receptor subtypes.3-Carboxy-pyrazolinalanine as a new scaffold for developing potent and selective NMDA receptor antagonists.Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Inspired by Nature: The 3-Halo-4,5-dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors.Engineering of α-conotoxin MII-derived peptides with increased selectivity for native α6β2* nicotinic acetylcholine receptors.Mechanism of falcipain-2 inhibition by α,β-unsaturated benzo[1,4]diazepin-2-one methyl ester.Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.
P50
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P50
description
onderzoeker
@nl
researcher
@en
հետազոտող
@hy
name
Carlo De Micheli
@ast
Carlo De Micheli
@en
Carlo De Micheli
@es
Carlo De Micheli
@nl
type
label
Carlo De Micheli
@ast
Carlo De Micheli
@en
Carlo De Micheli
@es
Carlo De Micheli
@nl
prefLabel
Carlo De Micheli
@ast
Carlo De Micheli
@en
Carlo De Micheli
@es
Carlo De Micheli
@nl
P1053
A-9656-2011
P106
P1153
7004045399
P21
P31
P3829
P496
0000-0003-3549-4365