Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Hermogenes N. Jimenez"'
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
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
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
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
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
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⟩
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
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
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
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
Autor:
Upendra P. Topiwala, Michael Konkel, Hermogenes N. Jimenez, Heidi Chen, Heather Coate, Mary W. Walker, Mathivanan Packiarajan, Ian Jamie Talisman
Publikováno v:
ChemInform. 37