Search Results - "Ceccarelli, Simona M"
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Carnitine Palmitoyltransferase (CPT) Modulators: A Medicinal Chemistry Perspective on 35 Years of Research
Published in Journal of medicinal chemistry (12-05-2011)Get full text
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2
Metabolite Identification via LC-SPE-NMR-MS of the In vitro Biooxidation Products of a Lead mGlu5 Allosteric Antagonist and Impact on the Improvement of Metabolic Stability in the Series
Published in ChemMedChem (11-01-2008)“…Detailed information on the metabolic fate of lead compounds can be a powerful tool for an informed approach to the stabilization of metabolically labile…”
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3
Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-10-2016)“…[Display omitted] Dual inhibition of fatty acid binding proteins 4 and 5 (FABP4 and FABP5) is expected to provide beneficial effects on a number of metabolic…”
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4
LC-SPE-NMR-MS: a total analysis system for bioanalysis
Published in Bioanalysis (01-06-2009)“…Liquid chromatography (LC)-solid-phase extraction (SPE)-nuclear magnetic resonance (NMR)-mass spectrometry (MS) coupling is a key technology for fast and…”
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5
Rational design, synthesis, and structure–activity relationship of benzoxazolones: New potent mglu5 receptor antagonists based on the fenobam structure
Published in Bioorganic & medicinal chemistry letters (01-03-2007)“…A novel class of potent and stable mGlu5 receptor antagonists was developed by combining information from a high-throughput screening campaign with the…”
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6
Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors
Published in Bioorganic & medicinal chemistry letters (15-01-2006)“…Screening of the Roche compound library led to the identification of cis- N-(2-phenyl-cyclohexyl)-spiropiperidine 1 as structurally novel GlyT1 inhibitor. The…”
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Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile
Published in Bioorganic & medicinal chemistry letters (15-01-2006)“…During SAR exploration of N-(2-aryl-cyclohexyl) substituted spiropiperidine as GlyT1 inhibitors, it was found that introduction of a hydroxy group in position…”
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Synthetic studies on the sarcodictyins: synthesis of fully functionalized cyclization precursors
Published in Tetrahedron (01-10-2001)“…A strategy featuring a key retrosynthetic disconnection at the C2–C3 position was applied to the total synthesis of the common diterpenoid tricyclic skeleton…”
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Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2007)“…Optimization of affinity and microsomal stability led to identification of the potent, metabolically stable fenobam analog 4l. Robust in vivo efficacy of 4l…”
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Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: Achieving selectivity against the μ opioid and nociceptin/orphanin FQ peptide (NOP) receptors
Published in Bioorganic & medicinal chemistry letters (15-08-2006)“…A novel class of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-ones have been discovered and developed as potent and selective GlyT1…”
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11
A carbonylative cross-coupling strategy to the total synthesis of the sarcodictyins: preliminary studies and synthesis of a cyclization precursor
Published in Tetrahedron letters (15-10-2001)“…Preliminary studies were conducted on the implementation of a new strategy to the total synthesis of the common diterpenoid tricyclic skeleton of sarcodictyins…”
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12
Synthesis of a simplified sarcodictyin analogue which retains microtubule stabilising properties
Published in Tetrahedron letters (24-12-2001)“…A strategy featuring ring-closing metathesis as key reaction is applied to the synthesis of the sarcodictyin analogue 15 . The precursor diene is accessed via…”
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