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Items: 26

1.

NF-κB activation in astrocytes drives a stage-specific beneficial neuroimmunological response in ALS.

Ouali Alami N, Schurr C, Olde Heuvel F, Tang L, Li Q, Tasdogan A, Kimbara A, Nettekoven M, Ottaviani G, Raposo C, Röver S, Rogers-Evans M, Rothenhäusler B, Ullmer C, Fingerle J, Grether U, Knuesel I, Boeckers TM, Ludolph A, Wirth T, Roselli F, Baumann B.

EMBO J. 2018 Jun 6. pii: e98697. doi: 10.15252/embj.201798697. [Epub ahead of print]

2.

Challenges and Rewards in Medicinal Chemistry Targeting Cardiovascular and Metabolic Diseases.

Neidhart W, Ackermann J, Amrein K, Conte A, Hunziker D, Kuhn B, Märki HP, Nettekoven M, Ruf A, Schulz-Gasch T, Mayweg AV.

Chimia (Aarau). 2015;69(7-8):407-13. doi: 10.2533/chimia.2015.407. Review.

PMID:
26507592
3.

Challenges and Rewards in Medicinal Chemistry Targeting Cardiovascular and Metabolic Diseases.

Neidhart W, Ackermann J, Amrein K, Conte A, Hunziker D, Kuhn B, Märki HP, Nettekoven M, Ruf A, Schulz-Gasch T, Mayweg AV.

Chimia (Aarau). 2015 Aug 19;69(7):407-413. doi: 10.2533/chimia.2015.407.

PMID:
28482972
4.

Novel Triazolopyrimidine-Derived Cannabinoid Receptor 2 Agonists as Potential Treatment for Inflammatory Kidney Diseases.

Nettekoven M, Adam JM, Bendels S, Bissantz C, Fingerle J, Grether U, Grüner S, Guba W, Kimbara A, Ottaviani G, Püllmann B, Rogers-Evans M, Röver S, Rothenhäusler B, Schmitt S, Schuler F, Schulz-Gasch T, Ullmer C.

ChemMedChem. 2016 Jan 19;11(2):179-89. doi: 10.1002/cmdc.201500218. Epub 2015 Jul 21.

PMID:
26228928
5.

6-Alkoxy-5-aryl-3-pyridinecarboxamides, a new series of bioavailable cannabinoid receptor type 1 (CB1) antagonists including peripherally selective compounds.

Röver S, Andjelkovic M, Bénardeau A, Chaput E, Guba W, Hebeisen P, Mohr S, Nettekoven M, Obst U, Richter WF, Ullmer C, Waldmeier P, Wright MB.

J Med Chem. 2013 Dec 27;56(24):9874-96. doi: 10.1021/jm4010708. Epub 2013 Nov 20.

PMID:
24175572
6.

Conformationally restricted pyrrolidines by intramolecular [2+2] photocycloaddition reactions.

Fort DA, Woltering TJ, Nettekoven M, Knust H, Bach T.

Chem Commun (Camb). 2013 Apr 14;49(29):2989-91. doi: 10.1039/c3cc40757h.

PMID:
23463393
7.

Highly potent and selective cannabinoid receptor 2 agonists: initial hit optimization of an adamantyl hit series identified from high-through-put screening.

Nettekoven M, Fingerle J, Grether U, Grüner S, Kimbara A, Püllmann B, Rogers-Evans M, Röver S, Schuler F, Schulz-Gasch T, Ullmer C.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1177-81. doi: 10.1016/j.bmcl.2013.01.044. Epub 2013 Jan 23.

PMID:
23380378
8.

Synthesis of fluorinated tricyclic scaffolds by intramolecular [2+2] photocycloaddition reactions.

Fort DA, Woltering TJ, Nettekoven M, Knust H, Bach T.

Angew Chem Int Ed Engl. 2012 Oct 1;51(40):10169-72. doi: 10.1002/anie.201204080. Epub 2012 Sep 7. No abstract available.

PMID:
22962009
9.

Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.

Ratni H, Ballard TM, Bissantz C, Hoffmann T, Jablonski P, Knoflach F, Knust H, Malherbe P, Nettekoven M, Patiny-Adam A, Riemer C, Schmitt M, Spooren W.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6735-8. doi: 10.1016/j.bmcl.2010.08.138. Epub 2010 Sep 17.

PMID:
20850972
10.

Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.

Richter HG, Freichel C, Huwyler J, Nakagawa T, Nettekoven M, Plancher JM, Raab S, Roche O, Schuler F, Taylor S, Ullmer C, Wiegand R.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5713-7. doi: 10.1016/j.bmcl.2010.08.009. Epub 2010 Aug 6.

PMID:
20801030
11.

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
12.

Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.

Malherbe P, Kratzeisen C, Marcuz A, Zenner MT, Nettekoven MH, Ratni H, Wettstein JG, Bissantz C.

J Med Chem. 2009 Nov 26;52(22):7103-12. doi: 10.1021/jm900948q.

PMID:
19817444
13.

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.

14.

Selective naphthalene H(3) receptor inverse agonists with reduced potential to induce phospholipidosis and their quinoline analogs.

Rodríguez Sarmiento RM, Nettekoven MH, Taylor S, Plancher JM, Richter H, Roche O.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4495-500. doi: 10.1016/j.bmcl.2009.03.100. Epub 2009 Mar 26.

PMID:
19524437
15.

5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.

Pierson PD, Fettes A, Freichel C, Gatti-McArthur S, Hertel C, Huwyler J, Mohr P, Nakagawa T, Nettekoven M, Plancher JM, Raab S, Richter H, Roche O, Rodríguez Sarmiento RM, Schmitt M, Schuler F, Takahashi T, Taylor S, Ullmer C, Wiegand R.

J Med Chem. 2009 Jul 9;52(13):3855-68. doi: 10.1021/jm900409x.

PMID:
19456097
16.

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
17.

Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.

Roche O, Nettekoven M, Vifian W, Sarmiento RM.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4377-9. doi: 10.1016/j.bmcl.2008.06.062. Epub 2008 Jun 21.

PMID:
18606542
18.

Benzodioxoles: novel cannabinoid-1 receptor inverse agonists for the treatment of obesity.

Alig L, Alsenz J, Andjelkovic M, Bendels S, Bénardeau A, Bleicher K, Bourson A, David-Pierson P, Guba W, Hildbrand S, Kube D, Lübbers T, Mayweg AV, Narquizian R, Neidhart W, Nettekoven M, Plancher JM, Rocha C, Rogers-Evans M, Röver S, Schneider G, Taylor S, Waldmeier P.

J Med Chem. 2008 Apr 10;51(7):2115-27. doi: 10.1021/jm701487t. Epub 2008 Mar 13.

PMID:
18335976
19.

Aminothiazole derivatives as neuropeptide Y5 receptor ligands: finding the balance between affinity and physicochemical properties.

Nettekoven M, Guba W, Neidhart W, Mattei P, Pflieger P, Plancher JM, Taylor S.

ChemMedChem. 2006 Jan;1(1):45-8. No abstract available.

PMID:
16892333
20.

Isomeric thiazole derivatives as ligands for the neuropeptide Y5 receptor.

Nettekoven M, Guba W, Neidhart W, Mattei P, Pflieger P, Roche O, Taylor S.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3446-9.

PMID:
15951170
21.

Novel and potent NPY5 receptor antagonists derived from virtual screening and iterative parallel chemistry design.

Guba W, Neidhart W, Nettekoven M.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1599-603.

PMID:
15745805
22.
23.
24.

Lead generation--enhancing the success of drug discovery by investing in the hit to lead process.

Alanine A, Nettekoven M, Roberts E, Thomas AW.

Comb Chem High Throughput Screen. 2003 Feb;6(1):51-66.

PMID:
12570752
25.

Accelerating drug discovery by integrative implementation of laboratory automation in the work flow.

Nettekoven M, Thomas AW.

Curr Med Chem. 2002 Dec;9(23):2179-90. Review.

PMID:
12470254
26.

Combinatorial synthesis of libraries of indole derivatives.

Nettekoven M.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2169-71.

PMID:
11514162

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