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Items: 1 to 50 of 97

1.

Applications of organocatalysed visible-light photoredox reactions for medicinal chemistry.

Bogdos MK, Pinard E, Murphy JA.

Beilstein J Org Chem. 2018 Aug 3;14:2035-2064. doi: 10.3762/bjoc.14.179. eCollection 2018. Review.

2.

Glycine Transporter Type I (GlyT1) Inhibitor, Bitopertin: A Journey from Lab to Patient.

Pinard E, Borroni E, Koerner A, Umbricht D, Alberati D.

Chimia (Aarau). 2018 Aug 22;72(7):477-484. doi: 10.2533/chimia.2018.477.

PMID:
30158010
3.

Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 ( SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA).

Ratni H, Ebeling M, Baird J, Bendels S, Bylund J, Chen KS, Denk N, Feng Z, Green L, Guerard M, Jablonski P, Jacobsen B, Khwaja O, Kletzl H, Ko CP, Kustermann S, Marquet A, Metzger F, Mueller B, Naryshkin NA, Paushkin SV, Pinard E, Poirier A, Reutlinger M, Weetall M, Zeller A, Zhao X, Mueller L.

J Med Chem. 2018 Aug 9;61(15):6501-6517. doi: 10.1021/acs.jmedchem.8b00741. Epub 2018 Jul 25.

PMID:
30044619
4.

Discovery of a Novel Class of Survival Motor Neuron 2 Splicing Modifiers for the Treatment of Spinal Muscular Atrophy.

Pinard E, Green L, Reutlinger M, Weetall M, Naryshkin NA, Baird J, Chen KS, Paushkin SV, Metzger F, Ratni H.

J Med Chem. 2017 May 25;60(10):4444-4457. doi: 10.1021/acs.jmedchem.7b00406. Epub 2017 May 4.

PMID:
28441483
5.

Specific Correction of Alternative Survival Motor Neuron 2 Splicing by Small Molecules: Discovery of a Potential Novel Medicine To Treat Spinal Muscular Atrophy.

Ratni H, Karp GM, Weetall M, Naryshkin NA, Paushkin SV, Chen KS, McCarthy KD, Qi H, Turpoff A, Woll MG, Zhang X, Zhang N, Yang T, Dakka A, Vazirani P, Zhao X, Pinard E, Green L, David-Pierson P, Tuerck D, Poirier A, Muster W, Kirchner S, Mueller L, Gerlach I, Metzger F.

J Med Chem. 2016 Jul 14;59(13):6086-100. doi: 10.1021/acs.jmedchem.6b00459. Epub 2016 Jul 6.

PMID:
27299419
6.

A Real-World Perspective on Molecular Design.

Kuhn B, Guba W, Hert J, Banner D, Bissantz C, Ceccarelli S, Haap W, Körner M, Kuglstatter A, Lerner C, Mattei P, Neidhart W, Pinard E, Rudolph MG, Schulz-Gasch T, Woltering T, Stahl M.

J Med Chem. 2016 May 12;59(9):4087-102. doi: 10.1021/acs.jmedchem.5b01875. Epub 2016 Feb 24.

PMID:
26878596
7.

3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.

Pinard E, Alberati D, Alvarez-Sanchez R, Brom V, Burner S, Fischer H, Hauser N, Kolczewski S, Lengyel J, Mory R, Saladin C, Schulz-Gasch T, Stalder H.

ACS Med Chem Lett. 2014 Feb 4;5(4):428-33. doi: 10.1021/ml500005m. eCollection 2014 Apr 10.

8.

BACE1 inhibitors: a head group scan on a series of amides.

Woltering TJ, Wostl W, Hilpert H, Rogers-Evans M, Pinard E, Mayweg A, Göbel M, Banner DW, Benz J, Travagli M, Pollastrini M, Marconi G, Gabellieri E, Guba W, Mauser H, Andreini M, Jacobsen H, Power E, Narquizian R.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4239-43. doi: 10.1016/j.bmcl.2013.05.003. Epub 2013 May 18.

PMID:
23735744
9.

β-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.

Hilpert H, Guba W, Woltering TJ, Wostl W, Pinard E, Mauser H, Mayweg AV, Rogers-Evans M, Humm R, Krummenacher D, Muser T, Schnider C, Jacobsen H, Ozmen L, Bergadano A, Banner DW, Hochstrasser R, Kuglstatter A, David-Pierson P, Fischer H, Polara A, Narquizian R.

J Med Chem. 2013 May 23;56(10):3980-95. doi: 10.1021/jm400225m. Epub 2013 May 2.

PMID:
23590342
10.

Spatial and temporal MRI profile of ischemic tissue after the acute stages of a permanent mouse model of stroke.

Bogaert-Buchmann A, Poittevin M, Po C, Dupont D, Sebrié C, Tomita Y, Trandinh A, Seylaz J, Pinard E, Méric P, Kubis N, Gillet B.

Open Neuroimag J. 2013;7:4-14. doi: 10.2174/1874440001307010004. Epub 2013 Feb 1.

11.

Catastrophic paradoxical embolus after hemodialysis access thrombectomy in a patient with a patent foramen ovale.

Pinard EA, Fazal S, Schussler JM.

Int Urol Nephrol. 2013 Aug;45(4):1215-7. doi: 10.1007/s11255-012-0141-0. Epub 2012 Feb 25.

PMID:
22367171
12.

Glycine reuptake inhibitor RG1678: a pharmacologic characterization of an investigational agent for the treatment of schizophrenia.

Alberati D, Moreau JL, Lengyel J, Hauser N, Mory R, Borroni E, Pinard E, Knoflach F, Schlotterbeck G, Hainzl D, Wettstein JG.

Neuropharmacology. 2012 Feb;62(2):1152-61. doi: 10.1016/j.neuropharm.2011.11.008. Epub 2011 Nov 27.

PMID:
22138164
13.

Inhibiting glycine transporter-1 facilitates cocaine-cue extinction and attenuates reacquisition of cocaine-seeking behavior.

Nic Dhonnchadha BÁ, Pinard E, Alberati D, Wettstein JG, Spealman RD, Kantak KM.

Drug Alcohol Depend. 2012 Apr 1;122(1-2):119-26. doi: 10.1016/j.drugalcdep.2011.09.017. Epub 2011 Oct 10.

14.

Long-term, repeated measurements of mouse cortical microflow at the same region of interest with high spatial resolution.

Tomita Y, Pinard E, Tran-Dinh A, Schiszler I, Kubis N, Tomita M, Suzuki N, Seylaz J.

Brain Res. 2011 Feb 4;1372:59-69. doi: 10.1016/j.brainres.2010.11.014. Epub 2010 Nov 25.

PMID:
21111717
15.

Discovery of benzoylisoindolines as a novel class of potent, selective and orally active GlyT1 inhibitors.

Pinard E, Alberati D, Bender M, Borroni E, Brom V, Burner S, Fischer H, Hainzl D, Halm R, Hauser N, Jolidon S, Lengyel J, Marty HP, Meyer T, Moreau JL, Mory R, Narquizian R, Norcross RD, Schmid P, Wermuth R, Zimmerli D.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6960-5. doi: 10.1016/j.bmcl.2010.09.124. Epub 2010 Oct 7.

PMID:
20974532
16.

Influence of methotrexate exposure on outcome in patients treated with MBVP chemotherapy for primary central nervous system lymphoma.

Blasco H, Senecal D, Le Gouge A, Pinard E, Benz-de Bretagne I, Colombat P, Hulot JS, Chatelut E, Le Guellec C.

Br J Clin Pharmacol. 2010 Sep;70(3):367-75. doi: 10.1111/j.1365-2125.2010.03712.x.

17.

Pharmacological evaluation of a novel assay for detecting glycine transporter 1 inhibitors and their antipsychotic potential.

Alberati D, Moreau JL, Mory R, Pinard E, Wettstein JG.

Pharmacol Biochem Behav. 2010 Dec;97(2):185-91. doi: 10.1016/j.pbb.2010.07.016. Epub 2010 Aug 1.

18.

Selective GlyT1 inhibitors: discovery of [4-(3-fluoro-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][5-methanesulfonyl-2-((S)-2,2,2-trifluoro-1-methylethoxy)phenyl]methanone (RG1678), a promising novel medicine to treat schizophrenia.

Pinard E, Alanine A, Alberati D, Bender M, Borroni E, Bourdeaux P, Brom V, Burner S, Fischer H, Hainzl D, Halm R, Hauser N, Jolidon S, Lengyel J, Marty HP, Meyer T, Moreau JL, Mory R, Narquizian R, Nettekoven M, Norcross RD, Puellmann B, Schmid P, Schmitt S, Stalder H, Wermuth R, Wettstein JG, Zimmerli D.

J Med Chem. 2010 Jun 24;53(12):4603-14. doi: 10.1021/jm100210p.

PMID:
20491477
19.

Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.

Malherbe P, Borroni E, Gobbi L, Knust H, Nettekoven M, Pinard E, Roche O, Rogers-Evans M, Wettstein JG, Moreau JL.

Br J Pharmacol. 2009 Apr;156(8):1326-41. doi: 10.1111/j.1476-5381.2009.00127.x.

20.

Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists.

Malherbe P, Borroni E, Pinard E, Wettstein JG, Knoflach F.

Mol Pharmacol. 2009 Sep;76(3):618-31. doi: 10.1124/mol.109.055152. Epub 2009 Jun 19.

PMID:
19542319
21.

Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.

Jolidon S, Alberati D, Dowle A, Fischer H, Hainzl D, Narquizian R, Norcross R, Pinard E.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5533-6. doi: 10.1016/j.bmcl.2008.09.005. Epub 2008 Sep 6.

PMID:
18805008
22.

Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors.

Pinard E, Alberati D, Borroni E, Fischer H, Hainzl D, Jolidon S, Moreau JL, Narquizian R, Nettekoven M, Norcross RD, Stalder H, Thomas AW.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5134-9. doi: 10.1016/j.bmcl.2008.07.086. Epub 2008 Jul 24.

PMID:
18752953
23.

Magnetic targeting of nanometric magnetic fluid loaded liposomes to specific brain intravascular areas: a dynamic imaging study in mice.

Rivière C, Martina MS, Tomita Y, Wilhelm C, Tran Dinh A, Ménager C, Pinard E, Lesieur S, Gazeau F, Seylaz J.

Radiology. 2007 Aug;244(2):439-48. Epub 2007 Jun 11.

PMID:
17562813
24.

Vascular fate of adipose tissue-derived adult stromal cells in the ischemic murine brain: A combined imaging-histological study.

Kubis N, Tomita Y, Tran-Dinh A, Planat-Benard V, André M, Karaszewski B, Waeckel L, Pénicaud L, Silvestre JS, Casteilla L, Seylaz J, Pinard E.

Neuroimage. 2007 Jan 1;34(1):1-11. Epub 2006 Oct 23.

PMID:
17056275
25.

Cerebral microcirculation shear stress levels determine Neisseria meningitidis attachment sites along the blood-brain barrier.

Mairey E, Genovesio A, Donnadieu E, Bernard C, Jaubert F, Pinard E, Seylaz J, Olivo-Marin JC, Nassif X, Duménil G.

J Exp Med. 2006 Aug 7;203(8):1939-50. Epub 2006 Jul 24.

26.

4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.

Alberati D, Hainzl D, Jolidon S, Kurt A, Pinard E, Thomas AW, Zimmerli D.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4321-5. Epub 2006 Jun 9.

PMID:
16762550
27.

Design and synthesis of 4-substituted-8-(2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of GlyT1 inhibitors: achieving selectivity against the mu opioid and nociceptin/orphanin FQ peptide (NOP) receptors.

Alberati D, Ceccarelli SM, Jolidon S, Krafft EA, Kurt A, Maier A, Pinard E, Stalder H, Studer D, Thomas AW, Zimmerli D.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4305-10. Epub 2006 Jun 9.

PMID:
16762548
28.

Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.

Alberati D, Hainzl D, Jolidon S, Krafft EA, Kurt A, Maier A, Pinard E, Thomas AW, Zimmerli D.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4311-5. Epub 2006 Jun 6.

PMID:
16757170
29.

In vivo imaging with cellular resolution of bone marrow cells transplanted into the ischemic brain of a mouse.

Tran-Dinh A, Kubis N, Tomita Y, Karaszewski B, Calando Y, Oudina K, Petite H, Seylaz J, Pinard E.

Neuroimage. 2006 Jul 1;31(3):958-67. Epub 2006 Mar 3. Erratum in: Neuroimage. 2006 Nov 15;33(3):1028. Dinh, Alexy Tran [corrected to Tran-Dinh, Alexy].

PMID:
16516498
30.

The mitochondrial effects of small organic ligands of BCL-2: sensitization of BCL-2-overexpressing cells to apoptosis by a pyrimidine-2,4,6-trione derivative.

Milanesi E, Costantini P, Gambalunga A, Colonna R, Petronilli V, Cabrelle A, Semenzato G, Cesura AM, Pinard E, Bernardi P.

J Biol Chem. 2006 Apr 14;281(15):10066-72. Epub 2006 Feb 14.

31.

Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.

Ceccarelli SM, Pinard E, Stalder H, Alberati D.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):354-7. Epub 2005 Oct 21.

PMID:
16246561
32.

Discovery of N-(2-aryl-cyclohexyl) substituted spiropiperidines as a novel class of GlyT1 inhibitors.

Pinard E, Ceccarelli SM, Stalder H, Alberati D.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):349-53. Epub 2005 Oct 21.

PMID:
16246557
33.

Long-term in vivo investigation of mouse cerebral microcirculation by fluorescence confocal microscopy in the area of focal ischemia.

Tomita Y, Kubis N, Calando Y, Tran Dinh A, Méric P, Seylaz J, Pinard E.

J Cereb Blood Flow Metab. 2005 Jul;25(7):858-67.

PMID:
15758950
34.

The voltage-dependent anion channel is the target for a new class of inhibitors of the mitochondrial permeability transition pore.

Cesura AM, Pinard E, Schubenel R, Goetschy V, Friedlein A, Langen H, Polcic P, Forte MA, Bernardi P, Kemp JA.

J Biol Chem. 2003 Dec 12;278(50):49812-8. Epub 2003 Sep 2.

35.

1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.

Alanine A, Bourson A, Büttelmann B, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3155-9.

PMID:
12951084
36.

4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.

Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.

Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.

PMID:
12729659
37.

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.

Büttelmann B, Alanine A, Bourson A, Gill R, Heitz MP, Mutel V, Pinard E, Trube G, Wyler R.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):829-32.

PMID:
12617901
38.

Pharmacological characterization of Ro 63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-methyl-D-aspartate antagonist.

Gill R, Alanine A, Bourson A, Buttelmann B, Fischer G, Heitz MP, Kew JN, Levet-Trafit B, Lorez HP, Malherbe P, Miss MT, Mutel V, Pinard E, Roever S, Schmitt M, Trube G, Wybrecht R, Wyler R, Kemp JA.

J Pharmacol Exp Ther. 2002 Sep;302(3):940-8.

PMID:
12183650
39.

4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.

Pinard E, Alanine A, Bourson A, Büttelmann B, Heitz M, Mutela Ramanjit Gill V, Trube G, Wyler R.

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2615-9.

PMID:
12182873
40.

Passage of spermidine across the blood-brain barrier in short recirculation periods following global cerebral ischemia: effects of mild hyperthermia.

Diler AS, Ziylan YZ, Uzum G, Lefauconnier JM, Seylaz J, Pinard E.

Neurosci Res. 2002 Aug;43(4):335-42.

PMID:
12135777
41.

Albumin therapy of transient focal cerebral ischemia: in vivo analysis of dynamic microvascular responses.

Belayev L, Pinard E, Nallet H, Seylaz J, Liu Y, Riyamongkol P, Zhao W, Busto R, Ginsberg MD.

Stroke. 2002 Apr;33(4):1077-84.

PMID:
11935064
42.

Penumbral microcirculatory changes associated with peri-infarct depolarizations in the rat.

Pinard E, Nallet H, MacKenzie ET, Seylaz J, Roussel S.

Stroke. 2002 Feb;33(2):606-12.

PMID:
11823677
43.

Effects of chronic L-NAME treatment on rat focal cerebral ischemia and cerebral vasoreactivity.

Sercombe R, Issertial O, Seylaz J, Pinard E.

Life Sci. 2001 Sep 28;69(19):2203-16.

PMID:
11669463
44.

Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.

Pinard E, Alanine A, Bourson A, Büttelmann B, Gill R, Heitz M, Jaeschke G, Mutel V, Trube G, Wyler R.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2173-6.

PMID:
11514163
45.

Dynamic cerebral microcirculatory changes in transient forebrain ischemia in rats: involvement of type I nitric oxide synthase.

Pinard E, Engrand N, Seylaz J.

J Cereb Blood Flow Metab. 2000 Dec;20(12):1648-58.

PMID:
11129781
47.
48.

Dynamic in vivo measurement of erythrocyte velocity and flow in capillaries and of microvessel diameter in the rat brain by confocal laser microscopy.

Seylaz J, Charbonné R, Nanri K, Von Euw D, Borredon J, Kacem K, Méric P, Pinard E.

J Cereb Blood Flow Metab. 1999 Aug;19(8):863-70.

PMID:
10458593
49.

[Physiopathology of cerebral ischemia].

Pinard E, Engrand N.

Ann Fr Anesth Reanim. 1999 May;18(5):574-82. Review. French.

PMID:
10427395
50.

Influence of the antioxidant quercetin in vivo on the level of nitric oxide determined by electron paramagnetic resonance in rat brain during global ischemia and reperfusion.

Shutenko Z, Henry Y, Pinard E, Seylaz J, Potier P, Berthet F, Girard P, Sercombe R.

Biochem Pharmacol. 1999 Jan 15;57(2):199-208.

PMID:
9890569

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