List of works - Carlo De Micheli

1-Aryl-6,7-methylenedioxy-3 H -quinazolin-4-ones as anticonvulsant agents

scientific article published on 01 December 2003

3-Carboxy-pyrazolinalanine as a new scaffold for developing potent and selective NMDA receptor antagonists

scientific article

A SIMPLE AND EFFICIENT SYNTHESIS OF GYKI 52466 AND GYKI 52895

A chemoenzymatic approach to the synthesis of the stereoisomers of a β-adrenergic receptor antagonist

A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester

A novel simplified synthesis of acivicin

A novel spirocyclic tropanyl-Δ²-isoxazoline derivative enhances citalopram and paroxetine binding to serotonin transporters as well as serotonin uptake

scientific article

Alpha7 nicotinic acetylcholine receptor agonists: prediction of their binding affinity through a molecular mechanics Poisson-Boltzmann surface area approach

scientific article published in November 2008

Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists

scientific article

Chemoenzymatic synthesis of acetyl (R)-(+)- and (S)-(−)-cycloserine

Chemoenzymatic synthesis of the enantiomers of desoxymuscarine

Chiral separation of muscarinic antagonists by capillary zone electrophoresis with cyclodextrin additives

Design and synthesis of novel isoxazole-based HDAC inhibitors

scientific article published on 30 June 2010

Design of 1-substituted 2-arylmethyl-4,5-methylenedioxybenzene derivatives as antiseizure agents.

scientific article

Design of novel conformationally restricted analogues of glutamic acid

Design, synthesis, and pharmacological characterization of novel spirocyclic quinuclidinyl-Δ2-isoxazoline derivatives as potent and selective agonists of α7 nicotinic acetylcholine receptors

scientific article

Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists

scientific article published in December 2004

Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit

scientific article published in August 2005

Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead

scientific article published on 15 November 2013

Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

scientific article

Drug discovery targeting amino acid racemases

scientific article

Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors

scientific article published on 01 March 2014

Enantiopure stereoisomeric homologues of glutamic acid: chemoenzymatic synthesis and assignment of their absolute configurations

Engineering of α-conotoxin MII-derived peptides with increased selectivity for native α6β2* nicotinic acetylcholine receptors

scientific article published on 21 July 2011

Folates in Trypanosoma brucei: achievements and opportunities

scientific article published on 24 September 2018

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis

scientific article published on 7 May 2013

Inspired by Nature: The 3-Halo-4,5-dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors

scientific article

Investigating the mechanism of substrate uptake and release in the glutamate transporter homologue Glt(Ph) through metadynamics simulations

scientific article

Investigation on the chemoenzymatic synthesis of threo- and erythro-β-hydroxy-l-glutamic acid derivatives

Mechanism of falcipain-2 inhibition by α,β-unsaturated benzo[1,4]diazepin-2-one methyl ester

scientific article published on 11 September 2012

Mechanism of inhibition of the glutamate transporter EAAC1 by the conformationally constrained glutamate analogue (+)-HIP-B

scientific article

Metal-hydride reduction of isoxazoline-3-carboxylate esters

NMR characterization and conformational analysis of a potent papain-family cathepsin L-like cysteine protease inhibitor with different behaviour in polar and apolar media

article

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 reupta

scientific article

New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists

scientific article

New analogues of oxotremorine and oxotremorine-M: estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes.

scientific article published in June 2000

New spirocyclic Δ²-isoxazoline derivatives related to selective agonists of α7 neuronal nicotinic acetylcholine receptors

scientific article

Nitrile oxides in medicinal chemistry-2. synthesis of the two enantiomers of dihydromuscimol

Nitrile oxides in medicinal chemistry. 5. Lipase PS-catalyzed resolution of a set of heterocyclic derivatives

Nitrile oxides in medicinal chemistry. 6. Enzymatic resolution of a set of bicyclic Δ2-isoxazolines

Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: design, synthesis, and pharmacological characterization

scientific article published on September 2010

Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.

scientific article published on 2 February 2007

Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes

scientific article

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

scientific article published in September 2002

Regioselective Preparation of Functionalized Isoxazoline Derivatives as Key Intermediates for the Synthesis of Selective N-Methyl-d-aspartate Receptor Antagonists

Stereoselective Synthesis of 4-Amino-3-hydroxy-4,5,6,6a-tetrahydro-3aH-cyclopenta[d]isoxazole-4-carboxylic Acid, a Conformationally Constrained Analogue of Aspartic Acid

article by Carlo De Micheli et al published 3 July 2007 in Synthesis

Stereoselectivities of mesitonitrile oxide cycloadditions to 7-substituted norbornadienes

Synthesis and Anticonvulsant Activity of Novel and Potent 2,3-Benzodiazepine AMPA/Kainate Receptor Antagonists

scientific article published on 01 October 1999

Synthesis and Pharmacological Characterization of Enantiomerically Pure Muscarinic Agonists: Difluoromuscarines

scientific article published on 01 March 1997

Synthesis and Pharmacological Evaluation of α4β2Nicotinic Ligands with a 3-Fluoropyrrolidine Nucleus

scientific article published on 16 April 2015

Synthesis and Pharmacology of a New AMPA−Kainate Receptor Agonist with Potent Convulsant Activity

scientific article published on 01 September 1998

Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones

scientific article published on 01 February 2001

Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids

scientific article

Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine

scientific article published in 1997

Synthesis and biological evaluation of CTP synthetase inhibitors as potential agents for the treatment of African trypanosomiasis

scientific article published on 2 August 2012

Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antiprotozoal agents

scientific article

Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.

scientific article

Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M.

scientific article published in August 1999

Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands

scientific article published in September 2003

Synthesis and in vitro/in vivo evaluation of the antitrypanosomal activity of 3-bromoacivicin, a potent CTP synthetase inhibitor

scientific article

Synthesis and pharmacological characterization at glutamate receptors of erythro- and threo-tricholomic acid and homologues thereof

scholarly article by Paola Conti et al published March 2007 in Tetrahedron

Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid

scientific article

Synthesis and pharmacological characterization of new chiral derivatives of muscarine and allo-muscarine.

scientific article published in August 2000

Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid

scientific article published on 27 January 2007

Synthesis and pharmacological investigation of cholinergic ligands structurally related to muscarone

scholarly article by Marco De Amici et al published March 1989 in European Journal of Medicinal Chemistry

Synthesis and pharmacological investigation of the 3-analogs of viminol

scholarly article by Marco De Amici et al published November 1988 in European Journal of Medicinal Chemistry

Synthesis and pharmacology of 3-hydroxy-delta2-isoxazoline-cyclopentane analogues of glutamic acid.

scientific article

Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors

scientific article published on 25 January 2014

Synthesis of 3-Hydroxy- and 3-Carboxy-Δ2-isoxazoline Amino Acids and Evaluation of Their Interaction with GABA Receptors and Transporters

Synthesis of Conformationally Constrained Glutamic Acid Homologues and Investigation of Their Pharmacological Profiles

scientific article published on 01 November 2007

Synthesis of Epibatidine-Related Δ2-Isoxazoline Derivatives and Evaluation of Their Binding Affinity at Neuronal Nicotinic Acetylcholine Receptors

Synthesis of enantiomerically pure HIP-A and HIP-B and investigation of their activity as inhibitors of excitatory amino acid transporters

Synthesis of enantiopure Delta2-isoxazoline derivatives and evaluation of their affinity and efficacy profiles at human beta-adrenergic receptor subtypes

scientific article published on 10 March 2006

Synthesis of new bicyclic analogues of glutamic acid

Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors

scientific article published on 23 December 2010

Synthesis of new β- and γ-benzyloxy-S-glutamic acid derivatives and evaluation of their activity as inhibitors of excitatory amino acid transporters

article published in 2009

Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes

scientific article published on 17 September 2010

Synthesis of novel pyrrolo[3,4-d]pyrazole-dicarboxylic acids and evaluation of their interaction with glutamate receptors

scientific article published in April 2008

Synthesis of unusual isoxazoline containing β and γ-dipeptides as potential glutamate receptor ligands

Synthesis, binding affinity at glutamic acid receptors, neuroprotective effects, and molecular modeling investigation of novel dihydroisoxazole amino acids

scientific article

The enantiomers of epiboxidine and of two related analogs: Synthesis and estimation of their binding affinity at α4β2 and α7 neuronal nicotinic acetylcholine receptors

List of works by Carlo De Micheli

1-Aryl-6,7-methylenedioxy-3 H -quinazolin-4-ones as anticonvulsant agents

3-Carboxy-pyrazolinalanine as a new scaffold for developing potent and selective NMDA receptor antagonists

A SIMPLE AND EFFICIENT SYNTHESIS OF GYKI 52466 AND GYKI 52895

A chemoenzymatic approach to the synthesis of the stereoisomers of a β-adrenergic receptor antagonist

A highly efficient flow reactor process for the synthesis of N-Boc-3,4-dehydro-l-proline methyl ester

A novel simplified synthesis of acivicin

A novel spirocyclic tropanyl-Δ²-isoxazoline derivative enhances citalopram and paroxetine binding to serotonin transporters as well as serotonin uptake

Alpha7 nicotinic acetylcholine receptor agonists: prediction of their binding affinity through a molecular mechanics Poisson-Boltzmann surface area approach

Characterization of the mechanism of anticonvulsant activity for a selected set of putative AMPA receptor antagonists

Chemoenzymatic synthesis of acetyl (R)-(+)- and (S)-(−)-cycloserine

Chemoenzymatic synthesis of the enantiomers of desoxymuscarine

Chiral separation of muscarinic antagonists by capillary zone electrophoresis with cyclodextrin additives

Design and synthesis of novel isoxazole-based HDAC inhibitors

Design of 1-substituted 2-arylmethyl-4,5-methylenedioxybenzene derivatives as antiseizure agents.

Design of novel conformationally restricted analogues of glutamic acid

Design, synthesis, and pharmacological characterization of novel spirocyclic quinuclidinyl-Δ2-isoxazoline derivatives as potent and selective agonists of α7 nicotinic acetylcholine receptors

Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists

Development of a three-dimensional model for the N-methyl-D-aspartate NR2A subunit

Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead

Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria

Drug discovery targeting amino acid racemases

Efficient synthesis of novel glutamate homologues and investigation of their affinity and selectivity profile at ionotropic glutamate receptors

Enantiopure stereoisomeric homologues of glutamic acid: chemoenzymatic synthesis and assignment of their absolute configurations

Engineering of α-conotoxin MII-derived peptides with increased selectivity for native α6β2* nicotinic acetylcholine receptors

Folates in Trypanosoma brucei: achievements and opportunities

Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis

Inspired by Nature: The 3-Halo-4,5-dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors

Investigating the mechanism of substrate uptake and release in the glutamate transporter homologue Glt(Ph) through metadynamics simulations

Investigation on the chemoenzymatic synthesis of threo- and erythro-β-hydroxy-l-glutamic acid derivatives

Mechanism of falcipain-2 inhibition by α,β-unsaturated benzo[1,4]diazepin-2-one methyl ester

Mechanism of inhibition of the glutamate transporter EAAC1 by the conformationally constrained glutamate analogue (+)-HIP-B

Metal-hydride reduction of isoxazoline-3-carboxylate esters

NMR characterization and conformational analysis of a potent papain-family cathepsin L-like cysteine protease inhibitor with different behaviour in polar and apolar media

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 reupta

New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists

New analogues of oxotremorine and oxotremorine-M: estimation of their in vitro affinity and efficacy at muscarinic receptor subtypes.

New spirocyclic Δ²-isoxazoline derivatives related to selective agonists of α7 neuronal nicotinic acetylcholine receptors

Nitrile oxides in medicinal chemistry-2. synthesis of the two enantiomers of dihydromuscimol

Nitrile oxides in medicinal chemistry. 5. Lipase PS-catalyzed resolution of a set of heterocyclic derivatives

Nitrile oxides in medicinal chemistry. 6. Enzymatic resolution of a set of bicyclic Δ2-isoxazolines

Novel 3-carboxy- and 3-phosphonopyrazoline amino acids as potent and selective NMDA receptor antagonists: design, synthesis, and pharmacological characterization

Novel chiral isoxazole derivatives: synthesis and pharmacological characterization at human beta-adrenergic receptor subtypes.

Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes

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

Regioselective Preparation of Functionalized Isoxazoline Derivatives as Key Intermediates for the Synthesis of Selective N-Methyl-d-aspartate Receptor Antagonists

Stereoselective Synthesis of 4-Amino-3-hydroxy-4,5,6,6a-tetrahydro-3aH-cyclopenta[d]isoxazole-4-carboxylic Acid, a Conformationally Constrained Analogue of Aspartic Acid

Stereoselectivities of mesitonitrile oxide cycloadditions to 7-substituted norbornadienes

Synthesis and Anticonvulsant Activity of Novel and Potent 2,3-Benzodiazepine AMPA/Kainate Receptor Antagonists

Synthesis and Pharmacological Characterization of Enantiomerically Pure Muscarinic Agonists: Difluoromuscarines

Synthesis and Pharmacological Evaluation of α4β2Nicotinic Ligands with a 3-Fluoropyrrolidine Nucleus

Synthesis and Pharmacology of a New AMPA−Kainate Receptor Agonist with Potent Convulsant Activity

Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones

Synthesis and anticonvulsant activity of novel bicyclic acidic amino acids

Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine

Synthesis and biological evaluation of CTP synthetase inhibitors as potential agents for the treatment of African trypanosomiasis

Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antiprotozoal agents

Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.

Synthesis and functional characterization of novel derivatives related to oxotremorine and oxotremorine-M.

Synthesis and in vitro pharmacology of novel heterocyclic muscarinic ligands

Synthesis and in vitro/in vivo evaluation of the antitrypanosomal activity of 3-bromoacivicin, a potent CTP synthetase inhibitor

Synthesis and pharmacological characterization at glutamate receptors of erythro- and threo-tricholomic acid and homologues thereof

Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid

Synthesis and pharmacological characterization of new chiral derivatives of muscarine and allo-muscarine.

Synthesis and pharmacological evaluation of novel conformationally constrained homologues of glutamic acid

Synthesis and pharmacological investigation of cholinergic ligands structurally related to muscarone

Synthesis and pharmacological investigation of the 3-analogs of viminol

Synthesis and pharmacology of 3-hydroxy-delta2-isoxazoline-cyclopentane analogues of glutamic acid.

Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors

Synthesis of 3-Hydroxy- and 3-Carboxy-Δ2-isoxazoline Amino Acids and Evaluation of Their Interaction with GABA Receptors and Transporters

Synthesis of Conformationally Constrained Glutamic Acid Homologues and Investigation of Their Pharmacological Profiles

Synthesis of Epibatidine-Related Δ2-Isoxazoline Derivatives and Evaluation of Their Binding Affinity at Neuronal Nicotinic Acetylcholine Receptors

Synthesis of enantiomerically pure HIP-A and HIP-B and investigation of their activity as inhibitors of excitatory amino acid transporters

Synthesis of enantiopure Delta2-isoxazoline derivatives and evaluation of their affinity and efficacy profiles at human beta-adrenergic receptor subtypes

Synthesis of new bicyclic analogues of glutamic acid

Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors

Synthesis of new β- and γ-benzyloxy-S-glutamic acid derivatives and evaluation of their activity as inhibitors of excitatory amino acid transporters

Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes

Synthesis of novel pyrrolo[3,4-d]pyrazole-dicarboxylic acids and evaluation of their interaction with glutamate receptors

Synthesis of unusual isoxazoline containing β and γ-dipeptides as potential glutamate receptor ligands