8 Result(s)
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Article
Rosario González-Muñiz
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Article
Open AccessHighly functionalized β-lactams and 2-ketopiperazines as TRPM8 antagonists with antiallodynic activity
The cool sensor transient receptor potential melastatin channel 8 (TRPM8) is highly expressed in trigeminal and dorsal root ganglia, playing a key role in cold hypersensitivity associated to different peripher...
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Open AccessSynthesis, high-throughput screening and pharmacological characterization of β–lactam derivatives as TRPM8 antagonists
The mammalian transient receptor potential melastatin channel 8 (TRPM8), highly expressed in trigeminal and dorsal root ganglia, mediates the cooling sensation and plays an important role in the cold hypersens...
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Article
2-Alkyl-2-carboxyazetidines as γ-turn inducers: incorporation into neurotrophin fragments
Conveniently substituted 2-alkyl-2-carboxyazetidine amino acids have been incorporated into NGF and NT3 tetrapeptide sequences to investigate their utility as reverse turn inducers (γ- vs. β-turns). Despite th...
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Exploring the binding pocket for pyridopyrimidine ligands at the CCK1 receptor by molecular docking
Pyridopyrimidine-based analogues are among the most highly potent and selective antagonists of cholecystokinin receptor subtype-1 (CCK1R) described to date. To better understand the structural and chemical fea...
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Exploring solid-phase approaches for the preparation of new β-lactams from amino acids
Two solid-phase approaches, involving the base-assisted intramolecularalkylation of N-chloroacetyl-Phe derivatives anchored to appropriatesolid supports, were investigated for the preparation of novel β-lactams. ...
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Studies on the synthesis of β-keto esters derived from dipeptides: search for a low-epimerizing method
β-Keto esters derived from dipeptides areprepared by application of common methodologiesemployed for the synthesis of amino acid-derivedβ-keto esters; however, epimerization of theC-terminal residue occurred t...
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Similarity Study on Peptide γ-turn Conformation Mimetics
The ability of a series of structures to mimic the geometric and electronic properties of an ideal γ–turn has been studied. Initially, an exhaustive conformational analysis was carried out using the molecular ...
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Article
Constrained C-terminal hexapeptide neurotensin analogues containing a 3-oxoindolizidine skeleton
In order to enforce different spatial orientations in the C-terminal hexapeptide of neurotensin (NT8−13) and to gain information about the importance of the 10–11 peptide bond for binding to NT receptors, the Pro
