Search Results - "PLAZZI, Pier Vincenzo"
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Synthesis and structure–activity relationships of a series of pyrrole cannabinoid receptor agonists
Published in Bioorganic & medicinal chemistry (01-09-2003)“…We designed and synthesized a series of pyrrole derivatives with the aim of investigating the structure–activity relationship (SAR) for the binding of…”
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Cyclohexylcarbamic Acid 3‘- or 4‘-Substituted Biphenyl-3-yl Esters as Fatty Acid Amide Hydrolase Inhibitors: Synthesis, Quantitative Structure−Activity Relationships, and Molecular Modeling Studies
Published in Journal of medicinal chemistry (07-10-2004)“…Fatty acid amide hydrolase (FAAH) is a promising target for modulating endocannabinoid and fatty acid ethanolamide signaling, which may have important…”
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MT2 selective melatonin receptor antagonists: design and structure-activity relationships
Published in ARKIVOC (19-04-2006)Get full text
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5-Benzylidene-hydantoins: Synthesis and antiproliferative activity on A549 lung cancer cell line
Published in European journal of medicinal chemistry (01-09-2009)“…Benzylidene hydantoins have been recently reported as a new class of EGFR inhibitors. We describe here a simple and efficient methodology for the parallel…”
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Design, Synthesis, and Structure−Activity Relationships of Alkylcarbamic Acid Aryl Esters, a New Class of Fatty Acid Amide Hydrolase Inhibitors
Published in Journal of medicinal chemistry (05-06-2003)“…Fatty acid amide hydrolase (FAAH), an intracellular serine hydrolase enzyme, participates in the deactivation of fatty acid ethanolamides such as the…”
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Synthesis and structure-activity relationships for biphenyl H3 receptor antagonists with moderate anti-cholinesterase activity
Published in Bioorganic & medicinal chemistry (01-12-2008)“…The combination of antagonism at histamine H(3) receptors and inhibition of acetylcholinesterase has been recently proposed as an approach to devise putative…”
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Analysis of Structure−Activity Relationships for MT2 Selective Antagonists by Melatonin MT1 and MT2 Receptor Models
Published in Journal of medicinal chemistry (16-06-2005)“…Three-dimensional homology models of human MT1 and MT2 melatonin receptors were built with the aim to investigate the structure−activity relationships (SARs)…”
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Synthesis and Structure-Activity Relationships of FAAH Inhibitors: Cyclohexylcarbamic Acid Biphenyl Esters with Chemical Modulation at the Proximal Phenyl Ring
Published in ChemMedChem (01-01-2006)“…Fatty acid amide hydrolase (FAAH) is a serine hydrolase that catalyzes the intracellular hydrolysis of fatty acid ethanolamides such as anandamide and…”
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Three-Dimensional Quantitative Structure−Activity Relationship Studies on Selected MT1 and MT2 Melatonin Receptor Ligands: Requirements for Subtype Selectivity and Intrinsic Activity Modulation
Published in Journal of medicinal chemistry (10-04-2003)“…The three-dimensional quantitative structure−activity relationship comparative molecular field analysis (3D-QSAR CoMFA) approach was applied to some classes of…”
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Synthesis, antioxidant activity and structure-activity relationships for a new series of 2-(N-acylaminoethyl)indoles with melatonin-like cytoprotective activity
Published in Journal of pineal research (01-04-2006)“…: 5‐Methoxy‐2‐(N‐acetylaminoethyl)indole (5d), a melatonin analogue derived from the transposition of the acetylaminoethyl side chain from C3 to C2 of the…”
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Indole-based analogs of melatonin: in vitro antioxidant and cytoprotective activities
Published in Journal of pineal research (01-03-2004)“…: The known neuroprotective actions of melatonin could be due to its antioxidant or radical scavenging activity, or they could be due to specific interactions…”
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Synthesis and Stability in Biological Media of 1H-Imidazole-1-carboxylates of ROS203, an Antagonist of the Histamine H3 Receptor
Published in Chemistry & biodiversity (01-01-2008)“…A series of carbamate derivatives of the H3 antagonist ROS203 (1) were prepared, and their lipophilicity and steric hindrance were modulated by introducing…”
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Melatonin Receptor Ligands: Synthesis of New Melatonin Derivatives and Comprehensive Comparative Molecular Field Analysis (CoMFA) Study
Published in Journal of medicinal chemistry (24-09-1998)“…The CoMFA methodology was applied to melatonin receptor ligands in order to establish quantitative structure−affinity relationships. One hundred thirty-three…”
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Melatonin
Published in Current medicinal chemistry (01-06-1999)“…Melatonin is the principal hormone secreted by the pineal gland, produced in humans with a circadian rhythm characterized by elevated blood levels during the…”
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Synthesis and biological evaluation of new non-imidazole H3-receptor antagonists of the 2-aminobenzimidazole series
Published in Bioorganic & medicinal chemistry (01-03-2006)“…A novel series of non-imidazole H(3)-receptor antagonists was developed, by chemical modification of a potent lead H(3)-antagonist composed by an imidazole…”
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Application of 3D-QSAR in the Rational Design of Receptor Ligands and Enzyme Inhibitors
Published in Chemistry & biodiversity (01-11-2005)“…Quantitative structure–activity relationships (QSARs) are frequently employed in medicinal chemistry projects, both to rationalize structure–activity…”
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5-Benzylidene-hydantoins as new EGFR inhibitors with antiproliferative activity
Published in Bioorganic & medicinal chemistry letters (01-08-2006)“…A series of 1,5-disubstituted hydantoins, whose structure was designed to interact at the ATP-binding site of EGFR, was synthesized and evaluated for…”
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Synthesis and structure–activity relationships for biphenyl H 3 receptor antagonists with moderate anti-cholinesterase activity
Published in Bioorganic & medicinal chemistry (01-12-2008)“…A series of H 3-antagonists with a 4,4′-biphenyl scaffold was developed, in which the terminal groups were modulated, providing compounds with high H 3…”
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Aryl azoles with neuroprotective activity—Parallel synthesis and attempts at target identification
Published in Bioorganic & medicinal chemistry (15-02-2008)“…A parallel synthesis of aryl azoles with neuroprotective activity is described. All compounds obtained were evaluated in a vitro assay using a NMDA toxicity…”
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Validation of a histamine H3 receptor model through structure-activity relationships for classical H3 antagonists
Published in Bioorganic & medicinal chemistry (01-10-2005)“…Histamine H(3) receptor is a G protein-coupled receptor whose activation inhibits the synthesis and release of histamine and other neurotransmitters from nerve…”
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