The Experts below are selected from a list of 4431 Experts worldwide ranked by ideXlab platform
Cosimo Altomare - One of the best experts on this subject based on the ideXlab platform.
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Discovery, Biological Evaluation, and Structure–Activity and −Selectivity Relationships of 6′-Substituted (E)‑2-(Benzofuran-3(2H)‑ylidene)‑N‑methylacetamides, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors
2016Co-Authors: Leonardo Pisani, Maria Barletta, Orazio Nicolotti, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Ramon Soto-otero, Estefania Mendez-alvarez, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high affinity toward both MAO isoforms. These novel MAO-Is may represent promising hits for the development of safer therapeutic agents with a potential against depression, PD, and other age-related neurodegenerative pathologies
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discovery biological evaluation and structure activity and selectivity relationships of 6 substituted e 2 benzofuran 3 2h ylidene n methylacetamides a novel class of potent and selective Monoamine Oxidase Inhibitors
Journal of Medicinal Chemistry, 2013Co-Authors: Leonardo Pisani, Maria Barletta, Ramon Sotootero, Orazio Nicolotti, Estefania Mendezalvarez, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high af...
Leonardo Pisani - One of the best experts on this subject based on the ideXlab platform.
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Discovery, Biological Evaluation, and Structure–Activity and −Selectivity Relationships of 6′-Substituted (E)‑2-(Benzofuran-3(2H)‑ylidene)‑N‑methylacetamides, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors
2016Co-Authors: Leonardo Pisani, Maria Barletta, Orazio Nicolotti, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Ramon Soto-otero, Estefania Mendez-alvarez, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high affinity toward both MAO isoforms. These novel MAO-Is may represent promising hits for the development of safer therapeutic agents with a potential against depression, PD, and other age-related neurodegenerative pathologies
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discovery biological evaluation and structure activity and selectivity relationships of 6 substituted e 2 benzofuran 3 2h ylidene n methylacetamides a novel class of potent and selective Monoamine Oxidase Inhibitors
Journal of Medicinal Chemistry, 2013Co-Authors: Leonardo Pisani, Maria Barletta, Ramon Sotootero, Orazio Nicolotti, Estefania Mendezalvarez, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high af...
Beth Levant - One of the best experts on this subject based on the ideXlab platform.
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Modulation of [3H]Quinpirole Binding in Brain By Monoamine Oxidase Inhibitors: Evidence For a Potential Novel Binding Site1
2016Co-Authors: Beth Levant, Kimberly A Morgan, Jeffrey D. Moehlenkamp, Neda L. Leonard, C. C. ChengAbstract:HJQuinpirole is a dopamine agonist with high affinity for the D2 and D3 dopamine receptor subtypes. A variety of drugs, most notably Monoamine Oxidase Inhibitors (MAOls), inhibit the bind-ing of [H]quinpirole, but not H]spiperone or [H1(-)-N-n-pro-pylnorapomorphine, in rat striatal membranes by a mechanism that does not appear to involve the enzymatic activity of MAO. This study extends the characterization of MAOI-displaceable [3H}quinpirole binding in rat brain. Clinically antidepressant MAOIs exhibited selectivity between sites labeled by [H]quin-pirole and H]spiperone as did a number of structurally related propargylamines and N-acylethylenediamine derivatives and other drugs such as debrisoquin and phenylbiguanide. The MAOIs clorgyline and Ro 41-1 049 were the most potent. Anti-depressant MAOls inhibited [H]quinpirole binding with the fol
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novel drug interactions at d2 dopamine receptors modulation of 3h quinpirole binding by Monoamine Oxidase Inhibitors
Life Sciences, 2002Co-Authors: Beth LevantAbstract:Abstract D 2 dopamine receptors are the principal target of drugs used to treat schizophrenia and Parkinson's disease. Recent findings suggest novel drug interactions at D 2 receptors, specifically interactions of Monoamine Oxidase Inhibitors (MAOIs) at a novel binding site that modulates the binding of [ 3 H]quinpirole to the D 2 receptor. That MAOIs inhibit [ 3 H]quinpirole binding challenges the traditional understanding of ligand interactions at dopamine receptors and may shed light on the mechanism of behavioral sensitization to psychostimulants and the pharmacology and toxicity of MAOIs.
Orazio Nicolotti - One of the best experts on this subject based on the ideXlab platform.
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Discovery, Biological Evaluation, and Structure–Activity and −Selectivity Relationships of 6′-Substituted (E)‑2-(Benzofuran-3(2H)‑ylidene)‑N‑methylacetamides, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors
2016Co-Authors: Leonardo Pisani, Maria Barletta, Orazio Nicolotti, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Ramon Soto-otero, Estefania Mendez-alvarez, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high affinity toward both MAO isoforms. These novel MAO-Is may represent promising hits for the development of safer therapeutic agents with a potential against depression, PD, and other age-related neurodegenerative pathologies
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discovery biological evaluation and structure activity and selectivity relationships of 6 substituted e 2 benzofuran 3 2h ylidene n methylacetamides a novel class of potent and selective Monoamine Oxidase Inhibitors
Journal of Medicinal Chemistry, 2013Co-Authors: Leonardo Pisani, Maria Barletta, Ramon Sotootero, Orazio Nicolotti, Estefania Mendezalvarez, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high af...
Antonellina Introcaso - One of the best experts on this subject based on the ideXlab platform.
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Discovery, Biological Evaluation, and Structure–Activity and −Selectivity Relationships of 6′-Substituted (E)‑2-(Benzofuran-3(2H)‑ylidene)‑N‑methylacetamides, a Novel Class of Potent and Selective Monoamine Oxidase Inhibitors
2016Co-Authors: Leonardo Pisani, Maria Barletta, Orazio Nicolotti, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Ramon Soto-otero, Estefania Mendez-alvarez, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high affinity toward both MAO isoforms. These novel MAO-Is may represent promising hits for the development of safer therapeutic agents with a potential against depression, PD, and other age-related neurodegenerative pathologies
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discovery biological evaluation and structure activity and selectivity relationships of 6 substituted e 2 benzofuran 3 2h ylidene n methylacetamides a novel class of potent and selective Monoamine Oxidase Inhibitors
Journal of Medicinal Chemistry, 2013Co-Authors: Leonardo Pisani, Maria Barletta, Ramon Sotootero, Orazio Nicolotti, Estefania Mendezalvarez, Marco Catto, Antonellina Introcaso, Angela Stefanachi, Saverio Cellamare, Cosimo AltomareAbstract:The use of selective Inhibitors of Monoamine Oxidase A (MAO-A) and B (MAO-B) holds a therapeutic relevance in the treatment of depressive disorders and Parkinson’s disease (PD), respectively. Here, the discovery of a new class of compounds acting as Monoamine Oxidase Inhibitors (MAO-Is) and bearing a 6′-substituted (E)-2-(benzofuran-3(2H)-ylidene)-N-alkylacetamide skeleton is reported. 6′-Sulfonyloxy derivatives exhibited outstanding affinities to MAO-A (7.0 nM < IC50 < 49 nM, much higher than moclobemide) and a pronounced MAO-A/B selectivity. The corresponding 6′-benzyloxy derivatives showed potent MAO-B inhibition and inverted selectivity profile. The rigid E-geometry of the exocyclic double bond allowed a more efficient binding conformation compared to more flexible and less active 2-(1-benzofuran-3-yl)-N-methylacetamide isomers and 4-N-methylcarboxamidomethylcoumarin analogues. Focused structural modifications and docking simulations enabled the identification of key molecular determinants for high af...