Výsledky vyhledávání - "Hermogenes N. Jimenez"

Discovery and structure–activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators

Autor: Dario Doller, Guiying Li, Hermogenes N. Jimenez, Robbin Brodbeck, Michelle A. Uberti, Daniel G. Smith, Hao Zhou, Jens Christian Madsen, Henrik Pedersen, Michel Grenon, Gamini Chandrasena, Sidney W. Topiol

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:1398-1406

A novel series of trans-1,3-cyclohexyl diamides was discovered and characterized as mGluR5 negative allosteric modulators (NAMs) lacking an alkyne moiety. Conformational constraint of one of the amide bonds in the diamide template led to a spirooxazo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6ab971983d6dcff5223bdaed66c13e9
https://doi.org/10.1016/j.bmcl.2012.12.078

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4-(1-Phenyl-1H-pyrazol-4-yl)quinolines as novel, selective and brain penetrant metabotropic glutamate receptor 4 positive allosteric modulators

Autor: Manuel Cajina, Megan Nattini, Michael Sabio, Michael S. Reitman, Dario Doller, Kevin G. Liu, Maria D. Bacolod, Hermogenes N. Jimenez, Sang-Phyo Hong, Michelle A. Uberti

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:3235-3239

4-(1-Phenyl-1H-pyrazol-4-yl)quinoline (1) was identified by screening the Lundbeck compound collection, and characterized as having mGlu4 receptor positive allosteric modulator properties. Compound 1 is selective over other mGlu receptors and a panel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b69b52a2908d3eaca5c8afd4f35dc6a
https://doi.org/10.1016/j.bmcl.2012.03.032

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Structure-Activity Relationships for Negative Allosteric mGluR5 Modulators

Autor: Søren Møller Nielsen, Hans Bräuner-Osborne, Ulf Madsen, Trine Kvist, Birgitte H. Kaae, Birgitte Nielsen, Hermogenes N. Jimenez, Kasper Harpsøe, Rasmus P. Clausen, Christina Mølck, Michelle A. Uberti, David E. Gloriam, Jesper Mosolff Mathiesen, Per Sauerberg

Publikováno v: ChemMedChem. 7:440-451

A series of compounds based on the mGluR5-selective ligand 2-methyl-6-(phenylethynyl)pyridine (MPEP) were designed and synthesized. The compounds were found to be either structural analogues of MPEP, substituted monomers, or dimeric analogues. All co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7774d86454abd58c47505cdaa9660566
https://doi.org/10.1002/cmdc.201100578

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Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility

Autor: Heidi Chen, Mary W. Walker, Ian Jamie Talisman, Upendra P. Topiwala, Michael Konkel, Mathivanan Packiarajan, Hermogenes N. Jimenez, Heather Coate

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 16:3950-3954

A series of amino analogs of 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (1) were synthesized to improve aqueous solubility, while retaining high affinity for the human galanin Gal3 receptor. A very potent analog (9e, 1,3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67bd6ada2e23a875d9560999a6487c5d
https://doi.org/10.1016/j.bmcl.2006.05.025

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Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

Autor: Søren Møller Nielsen, Kasper Harpsøe, Christina Mølck, Rasmus P. Clausen, Ulf Madsen, Lars Østergaard Pedersen, Hans Bräuner-Osborne, Hermogenes N. Jimenez, David E. Gloriam, Jesper Mosolff Mathiesen

Publikováno v: Molecular pharmacology. 82(5)

Metabotropic glutamate receptor subtype 5 (mGluR5) is a potential drug target in neurological and psychiatric disorders, and subtype-selective allosteric modulators have attracted much attention as potential drug candidates. In this study, the bindin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ddbdde09db9c30342f242b6527bf4bd
https://pubmed.ncbi.nlm.nih.gov/22899869

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Synergy between L-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: implications for Parkinson's disease treatment and dyskinesia

Autor: Lydia Kerkerian-Le Goff, Dario Doller, Christophe Melon, Khaled-Ezaheir Bennouar, Maria D. Bacolod, Hermogenes N. Jimenez, Paolo Gubellini, Manuel Cajina, Michelle A. Uberti

Publikováno v: Neuropharmacology
Neuropharmacology, 2013, 66, pp.158-69. ⟨10.1016/j.neuropharm.2012.03.022⟩
Neuropharmacology, Elsevier, 2013, 66, pp.158-69. ⟨10.1016/j.neuropharm.2012.03.022⟩

Group III metabotropic glutamate (mGlu) receptors are localized in presynaptic terminals within basal ganglia (BG) circuitry that become hyperactive due to dopamine depletion in Parkinson's disease (PD). For this reason, group III mGlu receptors, in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::130c4170b8541db9c1b59a920fbb96ba
https://pubmed.ncbi.nlm.nih.gov/22491024

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5-(2'-Pyridyl)-2-aminothiazoles: alkyl amino sulfonamides and sulfamides as potent NPY(5) antagonists

Autor: Mathivanan Packiarajan, Hermogenes N. Jimenez, Mary W. Walker, Mohammad R. Marzabadi, Kim Andersen, Mahesh N. Desai, Toni C. Wolinski, Emily Reinhard, Vrej Jubian, Heather Coate, Gamini Chandrasena

Publikováno v: Bioorganicmedicinal chemistry letters. 21(21)

Synthesis, SAR and physico-chemical properties of an alkyl aminothiazole series 8 and 16 are described. 2-Pyridylaminothiazole based compounds such as 8c and 16a exhibit high affinity at the NPY(5) receptor with desirable cLogPs and solubilities. How

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44107b81e368d97fb0a7f5bb5877e548
https://pubmed.ncbi.nlm.nih.gov/21924902

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6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators

Autor: Maria D. Bacolod, Hermogenes N. Jimenez, Dario Doller, Myriam April, Robb Brodbeck, Michelle A. Uberti, Weiss Jesse, Guiying Li

Publikováno v: Bioorganicmedicinal chemistry letters. 21(16)

A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterized by tractable SAR, good in vi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9605047c308e636bcec784ec6e57ab0f
https://pubmed.ncbi.nlm.nih.gov/21757343

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ChemInform Abstract: A New Method for the Synthesis of N-t-Butoxycarbonyl-Protected α- Alkoxy Amines from Allylamines Under Neutral Conditions

Autor: Hermogenes N. Jimenez, Hideo Nemoto, Yoshinori Yamamoto

Publikováno v: ChemInform. 22

Treatment of the Boc protected allylamines (4) with rhodium catalysts in the presence of alcohols produces N-Boc substituted α-alkoxy amines (5) in high yields, which can be used as a synthetic equivalents of activated imines having an easily deprot

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::abcc8114cbdba17a7491a8c438ddf83e
https://doi.org/10.1002/chin.199113132

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