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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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Article
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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Article
Microwave-assisted reaction of glycosylamine with aspartic acid
The synthesis of N-protected glycosyl amino acids from amines has been investigated and it was found that, under microwave conditions, glycosylamines could be hydrolyzed leading to new products containing a glyco...
