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Page 1
Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency.
Turlington M, Noetzel MJ, Bridges TM, Vinson PN, Steckler T, Lavreysen H, Mackie C, Bartolomé-Nebreda JM, Conde-Ceide S, Tong HM, Macdonald GJ, Daniels JS, Jones CK, Niswender CM, Conn PJ, Lindsley CW, Stauffer SR. Turlington M, et al. Among authors: macdonald gj. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3641-6. doi: 10.1016/j.bmcl.2014.04.087. Epub 2014 May 2. Bioorg Med Chem Lett. 2014. PMID: 24961642 Free PMC article.
N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.
Gregory KJ, Herman EJ, Ramsey AJ, Hammond AS, Byun NE, Stauffer SR, Manka JT, Jadhav S, Bridges TM, Weaver CD, Niswender CM, Steckler T, Drinkenburg WH, Ahnaou A, Lavreysen H, Macdonald GJ, Bartolomé JM, Mackie C, Hrupka BJ, Caron MG, Daigle TL, Lindsley CW, Conn PJ, Jones CK. Gregory KJ, et al. Among authors: macdonald gj. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. doi: 10.1124/jpet.113.206623. Epub 2013 Aug 21. J Pharmacol Exp Ther. 2013. PMID: 23965381 Free PMC article.
Scaffold hopping from pyridones to imidazo[1,2-a]pyridines. New positive allosteric modulators of metabotropic glutamate 2 receptor.
Tresadern G, Cid JM, Macdonald GJ, Vega JA, de Lucas AI, García A, Matesanz E, Linares ML, Oehlrich D, Lavreysen H, Biesmans I, Trabanco AA. Tresadern G, et al. Among authors: macdonald gj. Bioorg Med Chem Lett. 2010 Jan 1;20(1):175-9. doi: 10.1016/j.bmcl.2009.11.008. Epub 2009 Nov 10. Bioorg Med Chem Lett. 2010. PMID: 19932615
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.
Trabanco AA, Duvey G, Cid JM, Macdonald GJ, Cluzeau P, Nhem V, Furnari R, Behaj N, Poulain G, Finn T, Lavreysen H, Poli S, Raux A, Thollon Y, Poirier N, D'Addona D, Andrés JI, Lutjens R, Le Poul E, Imogai H, Rocher JP. Trabanco AA, et al. Among authors: macdonald gj. Bioorg Med Chem Lett. 2011 Feb 1;21(3):971-6. doi: 10.1016/j.bmcl.2010.12.048. Epub 2010 Dec 21. Bioorg Med Chem Lett. 2011. PMID: 21232953
Imidazo[1,2-a]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor.
Trabanco AA, Tresadern G, Macdonald GJ, Vega JA, de Lucas AI, Matesanz E, García A, Linares ML, Alonso de Diego SA, Alonso JM, Oehlrich D, Ahnaou A, Drinkenburg W, Mackie C, Andrés JI, Lavreysen H, Cid JM. Trabanco AA, et al. Among authors: macdonald gj. J Med Chem. 2012 Mar 22;55(6):2688-701. doi: 10.1021/jm201561r. Epub 2012 Mar 1. J Med Chem. 2012. PMID: 22352782
Discovery of 1,4-disubstituted 3-cyano-2-pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.
Cid JM, Duvey G, Tresadern G, Nhem V, Furnari R, Cluzeau P, Vega JA, de Lucas AI, Matesanz E, Alonso JM, Linares ML, Andrés JI, Poli SM, Lutjens R, Himogai H, Rocher JP, Macdonald GJ, Oehlrich D, Lavreysen H, Ahnaou A, Drinkenburg W, Mackie C, Trabanco AA. Cid JM, et al. Among authors: macdonald gj. J Med Chem. 2012 Mar 8;55(5):2388-405. doi: 10.1021/jm2016864. Epub 2012 Feb 24. J Med Chem. 2012. PMID: 22364337
Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover.
Manka JT, Vinson PN, Gregory KJ, Zhou Y, Williams R, Gogi K, Days E, Jadhav S, Herman EJ, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Steckler T, Daniels JS, Weaver CD, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Manka JT, et al. Among authors: macdonald gj. Bioorg Med Chem Lett. 2012 Oct 15;22(20):6481-5. doi: 10.1016/j.bmcl.2012.08.043. Epub 2012 Aug 24. Bioorg Med Chem Lett. 2012. PMID: 22981332 Free PMC article.
Discovery of 3-cyclopropylmethyl-7-(4-phenylpiperidin-1-yl)-8-trifluoromethyl[1,2,4]triazolo[4,3-a]pyridine (JNJ-42153605): a positive allosteric modulator of the metabotropic glutamate 2 receptor.
Cid JM, Tresadern G, Vega JA, de Lucas AI, Matesanz E, Iturrino L, Linares ML, Garcia A, Andrés JI, Macdonald GJ, Oehlrich D, Lavreysen H, Megens A, Ahnaou A, Drinkenburg W, Mackie C, Pype S, Gallacher D, Trabanco AA. Cid JM, et al. Among authors: macdonald gj. J Med Chem. 2012 Oct 25;55(20):8770-89. doi: 10.1021/jm3010724. Epub 2012 Oct 16. J Med Chem. 2012. PMID: 23072213
Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.
Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR. Rodriguez AL, et al. Among authors: macdonald gj. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7388-92. doi: 10.1016/j.bmcl.2012.10.068. Epub 2012 Oct 23. Bioorg Med Chem Lett. 2012. PMID: 23142615 Free PMC article.
240 results