Search Results - "Morera, Ludovica"
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Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds
Published in Bioorganic & medicinal chemistry letters (15-05-2012)“…A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels…”
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Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy
Published in Clinical epigenetics (24-05-2016)“…The term epigenetics is defined as heritable changes in gene expression that are not due to alterations of the DNA sequence. In the last years, it has become…”
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Synthesis and biological evaluation of [6]-gingerol analogues as transient receptor potential channel TRPV1 and TRPA1 modulators
Published in Bioorganic & medicinal chemistry letters (15-02-2012)“…In order to explore the structural determinants for the TRPV1 and TRPA1 agonist properties of gingerols, a series of nineteen analogues (1b–5) of racemic…”
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Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid CB 1 Receptor
Published in Journal of medicinal chemistry (14-06-2012)Get full text
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Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid CB1 Receptor
Published in Journal of medicinal chemistry (14-06-2012)“…We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modulators of the CB1 receptor. The presence of the carboxamide…”
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Development and characterization of endocannabinoid hydrolases FAAH and MAGL inhibitors bearing a benzotriazol-1-yl carboxamide scaffold
Published in Bioorganic & medicinal chemistry (01-11-2012)“…A series of (1H-benzo[d][1,2,3]triazol-1-yl)(4-benzylpiperazin-1-yl)methanones and of (1H-benzo[d][1,2,3]triazol-1-yl)(4-phenylpiperazin-1-yl)methanones has…”
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Biaryl tetrazolyl ureas as inhibitors of endocannabinoid metabolism: Modulation at the N-portion and distal phenyl ring
Published in European journal of medicinal chemistry (01-05-2013)“…In the present study, we have further extended the structure–activity relationships for the tetrazolyl ureas class of compounds as potential FAAH and/or MAGL…”
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(−)-Menthylamine derivatives as potent and selective antagonists of transient receptor potential melastatin type-8 (TRPM8) channels
Published in Bioorganic & medicinal chemistry letters (01-05-2010)“…The evaluation of a series of (−)-menthylamine derivatives led to the identification of some potent TRPM8 antagonists with IC 50 values versus icilin and…”
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4-Biphenylalanine- and 3-Phenyltyrosine-Derived Hydroxamic Acids as Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A
Published in ChemMedChem (20-09-2016)“…Overexpression of the histone lysine demethylase KDM4A, which regulates H3K9 and H3K36 methylation states, has been related to the pathology of several human…”
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2-(Alkyl/Aryl)Amino-6-Benzylpyrimidin-4(3H)-ones as Inhibitors of Wild-Type and Mutant HIV-1: Enantioselectivity Studies
Published in Journal of medicinal chemistry (12-04-2012)“…The single enantiomers of two pyrimidine-based HIV-1 non-nucleoside reverse transcriptase inhibitors, 1 (MC1501) and 2 (MC2082), were tested in both cellular…”
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Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands
Published in Bioorganic & medicinal chemistry letters (01-12-2009)“…The evaluation of a series of piperazinyl carbamates and ureas, designed on the basis of previously reported TRPV1 antagonists and FAAH inhibitors, led to the…”
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