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Items: 1 to 20 of 93

1.

GPR103 antagonists demonstrating anorexigenic activity in vivo: design and development of pyrrolo[2,3-c]pyridines that mimic the C-terminal Arg-Phe motif of QRFP26.

Georgsson J, Bergström F, Nordqvist A, Watson MJ, Blundell CD, Johansson MJ, Petersson AU, Yuan ZQ, Zhou Y, Kristensson L, Kakol-Palm D, Tyrchan C, Wellner E, Bauer U, Brodin P, Svensson Henriksson A.

J Med Chem. 2014 Jul 24;57(14):5935-48. doi: 10.1021/jm401951t. Epub 2014 Jul 2. Erratum in: J Med Chem. 2015 May 14;58(9):4086.

PMID:
24937104
2.

Correction to GPR103 Antagonists Demonstrating Anorexigenic Activity in Vivo: Design and Development of Pyrrolo[2,3-c]pyridines That Mimic the C-Terminal Arg-Phe Motif of QRFP26.

Georgsson J, Bergström F, Nordqvist A, Watson MJ, Blundell CD, Johansson MJ, Petersson AU, Yuan ZQ, Zhou Y, Kristensson L, Kakol-Palm D, Tyrchan C, Wellner E, Bauer U, Brodin P, Svensson Henriksson A.

J Med Chem. 2015 May 14;58(9):4086. doi: 10.1021/acs.jmedchem.5b00479. Epub 2015 Apr 15. No abstract available.

PMID:
25875054
3.

Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.

Hu YJ, St-Onge M, Laliberté S, Vallée F, Jin S, Bedard L, Labrecque J, Albert JS.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3199-203. doi: 10.1016/j.bmcl.2014.04.045. Epub 2014 Apr 19.

PMID:
24835202
4.

Molecular basis of agonist docking in a human GPR103 homology model by site-directed mutagenesis and structure-activity relationship studies.

Neveu C, Dulin F, Lefranc B, Galas L, Calbrix C, Bureau R, Rault S, Chuquet J, Boutin JA, Guilhaudis L, Ségalas-Milazzo I, Vaudry D, Vaudry H, Santos JS, Leprince J.

Br J Pharmacol. 2014 Oct;171(19):4425-39. doi: 10.1111/bph.12808. Epub 2014 Sep 5.

5.

3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.

Bignan GC, Battista K, Connolly PJ, Orsini MJ, Liu J, Middleton SA, Reitz AB.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. Epub 2006 Apr 24.

PMID:
16632355
6.

Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase.

Patnaik S, Stevens KL, Gerding R, Deanda F, Shotwell JB, Tang J, Hamajima T, Nakamura H, Leesnitzer MA, Hassell AM, Shewchuck LM, Kumar R, Lei H, Chamberlain SD.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):3136-40. doi: 10.1016/j.bmcl.2008.12.110. Epub 2009 Jan 6.

PMID:
19394223
7.

Synthesis and antiviral activity of an imidazo[1,2-a]pyrrolo[2,3-c]pyridine series against the bovine viral diarrhea virus.

Chezal JM, Paeshuyse J, Gaumet V, Canitrot D, Maisonial A, Lartigue C, Gueiffier A, Moreau E, Teulade JC, Chavignon O, Neyts J.

Eur J Med Chem. 2010 May;45(5):2044-7. doi: 10.1016/j.ejmech.2010.01.023. Epub 2010 Jan 20.

PMID:
20149501
8.

New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

Stauffer F, Furet P, Floersheimer A, Lang M.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1860-3. doi: 10.1016/j.bmcl.2012.01.076. Epub 2012 Jan 28.

PMID:
22335894
9.

New Hits as Antagonists of GPR103 Identified by HTS.

Nordqvist A, Kristensson L, Johansson KE, Isaksson da Silva K, Fex T, Tyrchan C, Svensson Henriksson A, Nilsson K.

ACS Med Chem Lett. 2014 Feb 22;5(5):527-32. doi: 10.1021/ml400519h. eCollection 2014 May 8.

10.
11.

Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.

Di Fabio R, Arban R, Bernasconi G, Braggio S, Blaney FE, Capelli AM, Castiglioni E, Donati D, Fazzolari E, Ratti E, Feriani A, Contini S, Gentile G, Ghirlanda D, Sabbatini FM, Andreotti D, Spada S, Marchioro C, Worby A, St-Denis Y.

J Med Chem. 2008 Nov 27;51(22):7273-86. doi: 10.1021/jm800743q.

PMID:
18975927
12.

Rational design of a low molecular weight, stable, potent, and long-lasting GPR103 aza-β3-pseudopeptide agonist.

Neveu C, Lefranc B, Tasseau O, Do-Rego JC, Bourmaud A, Chan P, Bauchat P, Le Marec O, Chuquet J, Guilhaudis L, Boutin JA, Ségalas-Milazzo I, Costentin J, Vaudry H, Baudy-Floc'h M, Vaudry D, Leprince J.

J Med Chem. 2012 Sep 13;55(17):7516-24. doi: 10.1021/jm300507d. Epub 2012 Aug 17.

PMID:
22800498
13.

Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists.

Di Fabio R, St-Denis Y, Sabbatini FM, Andreotti D, Arban R, Bernasconi G, Braggio S, Blaney FE, Capelli AM, Castiglioni E, Di Modugno E, Donati D, Fazzolari E, Ratti E, Feriani A, Contini S, Gentile G, Ghirlanda D, Provera S, Marchioro C, Roberts KL, Mingardi A, Mattioli M, Nalin A, Pavone F, Spada S, Trist DG, Worby A.

J Med Chem. 2008 Dec 11;51(23):7370-9. doi: 10.1021/jm800744m.

PMID:
18989952
14.

Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.

Wilczynski A, Wang XS, Joseph CG, Xiang Z, Bauzo RM, Scott JW, Sorensen NB, Shaw AM, Millard WJ, Richards NG, Haskell-Luevano C.

J Med Chem. 2004 Apr 22;47(9):2194-207.

PMID:
15084118
15.
16.

Synthesis, antimalarial activity, and molecular modeling of new pyrrolo[1,2-a]quinoxalines, bispyrrolo[1,2-a]quinoxalines, bispyrido[3,2-e]pyrrolo[1,2-a]pyrazines, and bispyrrolo[1,2-a]thieno[3,2-e]pyrazines.

Guillon J, Grellier P, Labaied M, Sonnet P, Léger JM, Déprez-Poulain R, Forfar-Bares I, Dallemagne P, Lemaître N, Péhourcq F, Rochette J, Sergheraert C, Jarry C.

J Med Chem. 2004 Apr 8;47(8):1997-2009.

PMID:
15055999
17.

Novel pyrazolo-tetrahydropyridines as potent orexin receptor antagonists.

Sifferlen T, Boss C, Cottreel E, Koberstein R, Gude M, Aissaoui H, Weller T, Gatfield J, Brisbare-Roch C, Jenck F.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1539-42. doi: 10.1016/j.bmcl.2010.01.070. Epub 2010 Jan 22.

PMID:
20144866
18.

3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.

Kulagowski JJ, Broughton HB, Curtis NR, Mawer IM, Ridgill MP, Baker R, Emms F, Freedman SB, Marwood R, Patel S, Patel S, Ragan CI, Leeson PD.

J Med Chem. 1996 May 10;39(10):1941-2. No abstract available.

PMID:
8642550
19.

5-Substituted 1H-pyrrolo[3,2-b]pyridines as inhibitors of gastric acid secretion.

Palmer AM, Münch G, Brehm C, Zimmermann PJ, Buhr W, Feth MP, Simon WA.

Bioorg Med Chem. 2008 Feb 1;16(3):1511-30. Epub 2007 Oct 12.

PMID:
17962023
20.

Synthesis of new pyrrolo[2,3-d]pyrimidine derivatives as antibacterial and antifungal agents.

Hilmy KM, Khalifa MM, Hawata MA, Keshk RM, el-Torgman AA.

Eur J Med Chem. 2010 Nov;45(11):5243-50. doi: 10.1016/j.ejmech.2010.08.043. Epub 2010 Aug 24.

PMID:
20828885

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