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Items: 1 to 20 of 111

1.

Fused thiazolyl alkynes as potent mGlu5 receptor positive allosteric modulators.

Packiarajan M, Grenon M, Zorn S, Hopper AT, White AD, Chandrasena G, Pu X, Brodbeck RM, Robichaud AJ.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4037-43. doi: 10.1016/j.bmcl.2013.05.070. Epub 2013 May 30.

PMID:
23770058
2.

Discovery of (1R,2R)-N-(4-(6-isopropylpyridin-2-yl)-3-(2-methyl-2H-indazol-5-yl)isothiazol-5-yl)-2-methylcyclopropanecarboxamide, a potent and orally efficacious mGlu5 receptor negative allosteric modulator.

Hao J, Dehlinger V, Fivush AM, Rudyk HC, Britton TC, Hollinshead SP, Vokits BP, Clark BP, Henry SS, Massey SM, Peng L, Dressman BA, Heinz BA, Roberts EF, Bracey-Walker MR, Swanson S, Catlow JT, Love PL, Tepool AD, Peters SC, Simmons RM, Iyengar S, McKinzie DL, Monn JA.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1249-52. doi: 10.1016/j.bmcl.2013.01.009. Epub 2013 Jan 12.

PMID:
23374867
3.

SAR studies on mGlu5 receptor positive allosteric modulators (2003- 2013).

Hao J, Xiong H.

Curr Top Med Chem. 2014;14(15):1789-841. Review.

PMID:
25176124
4.

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254).

Turlington M, Noetzel MJ, Chun A, Zhou Y, Gogliotti RD, Nguyen ED, Gregory KJ, Vinson PN, Rook JM, Gogi KK, Xiang Z, Bridges TM, Daniels JS, Jones C, Niswender CM, Meiler J, Conn PJ, Lindsley CW, Stauffer SR.

J Med Chem. 2013 Oct 24;56(20):7976-96. doi: 10.1021/jm401028t. Epub 2013 Oct 9.

5.

Azetidinyl oxadiazoles as potent mGluR5 positive allosteric modulators.

Packiarajan M, Ferreira CG, Hong SP, White AD, Chandrasena G, Pu X, Brodbeck RM, Robichaud AJ.

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6469-74. doi: 10.1016/j.bmcl.2012.08.044. Epub 2012 Aug 25.

PMID:
22975301
6.

Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators.

Zhou H, Topiol SW, Grenon M, Jimenez HN, Uberti MA, Smith DG, Brodbeck RM, Chandrasena G, Pedersen H, Madsen JC, Doller D, Li G.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1398-406. doi: 10.1016/j.bmcl.2012.12.078. Epub 2013 Jan 5.

PMID:
23357634
7.

Dihydrothiazolopyridone derivatives as a novel family of positive allosteric modulators of the metabotropic glutamate 5 (mGlu5) receptor.

Bartolomé-Nebreda JM, Conde-Ceide S, Delgado F, Iturrino L, Pastor J, Pena MÁ, Trabanco AA, Tresadern G, Wassvik CM, Stauffer SR, Jadhav S, Gogi K, Vinson PN, Noetzel MJ, Days E, Weaver CD, Lindsley CW, Niswender CM, Jones CK, Conn PJ, Rombouts F, Lavreysen H, Macdonald GJ, Mackie C, Steckler T.

J Med Chem. 2013 Sep 26;56(18):7243-59. doi: 10.1021/jm400650w. Epub 2013 Sep 4.

8.

Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.

Chae E, Shin YJ, Ryu EJ, Ji MK, Ryune Cho N, Lee KH, Jeong HJ, Kim SJ, Choi Y, Seok Oh K, Park CE, Soo Yoon Y.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2134-9. doi: 10.1016/j.bmcl.2013.01.116. Epub 2013 Feb 4.

PMID:
23434029
9.

Insights into the interaction of negative allosteric modulators with the metabotropic glutamate receptor 5: discovery and computational modeling of a new series of ligands with nanomolar affinity.

Anighoro A, Graziani D, Bettinelli I, Cilia A, De Toma C, Longhi M, Mangiarotti F, Menegon S, Pirona L, Poggesi E, Riva C, Rastelli G.

Bioorg Med Chem. 2015 Jul 1;23(13):3040-58. doi: 10.1016/j.bmc.2015.05.008. Epub 2015 May 12.

PMID:
26014480
10.

Synthesis and biological evaluation of picolinamides and thiazole-2-carboxamides as mGluR5 (metabotropic glutamate receptor 5) antagonists.

Vu HN, Kim JY, Hassan AH, Choi K, Park JH, Park KD, Lee JK, Pae AN, Choo H, Min SJ, Cho YS.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):140-4. doi: 10.1016/j.bmcl.2015.11.012. Epub 2015 Nov 5.

PMID:
26598462
11.

A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core.

Duvey G, Perry B, Le Poul E, Poli S, Bonnet B, Lambeng N, Charvin D, Donovan-Rodrigues T, Haddouk H, Gagliardi S, Rocher JP.

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4523-7. doi: 10.1016/j.bmcl.2013.06.044. Epub 2013 Jun 25.

PMID:
23850200
12.

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety.

Felts AS, Rodriguez AL, Morrison RD, Venable DF, Manka JT, Bates BS, Blobaum AL, Byers FW, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5779-85. doi: 10.1016/j.bmcl.2013.09.001. Epub 2013 Sep 10.

13.

4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.

Xiong H, Brugel TA, Balestra M, Brown DG, Brush KA, Hightower C, Hinkley L, Hoesch V, Kang J, Koether GM, McCauley JP Jr, McLaren FM, Panko LM, Simpson TR, Smith RW, Woods JM, Brockel B, Chhajlani V, Gadient RA, Spear N, Sygowski LA, Zhang M, Arora J, Breysse N, Wilson JM, Isaac M, Slassi A, King MM.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7381-4. doi: 10.1016/j.bmcl.2010.10.036. Epub 2010 Oct 21.

PMID:
21067920
14.

Discovery and SAR of novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5).

Martín-Martín ML, Bartolomé-Nebreda JM, Conde-Ceide S, Alonso de Diego SA, López S, Martínez-Viturro CM, Tong HM, Lavreysen H, Macdonald GJ, Steckler T, Mackie C, Bridges TM, Daniels JS, Niswender CM, Noetzel MJ, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1310-7. doi: 10.1016/j.bmcl.2015.01.038. Epub 2015 Jan 28.

15.

Computational analysis of negative and positive allosteric modulator binding and function in metabotropic glutamate receptor 5 (in)activation.

Dalton JA, Gómez-Santacana X, Llebaria A, Giraldo J.

J Chem Inf Model. 2014 May 27;54(5):1476-87. doi: 10.1021/ci500127c. Epub 2014 May 13.

PMID:
24793143
16.

Metabotropic glutamate receptor 5-positive allosteric modulators for the treatment of schizophrenia (2004-2012).

Lindsley CW, Stauffer SR.

Pharm Pat Anal. 2013 Jan;2(1):93-108. doi: 10.4155/ppa.12.82. Review.

PMID:
24236973
17.

Computer-aided design of negative allosteric modulators of metabotropic glutamate receptor 5 (mGluR5): Comparative molecular field analysis of aryl ether derivatives.

Selvam C, Thilagavathi R, Narasimhan B, Kumar P, Jordan BC, Ranganna K.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1140-4. doi: 10.1016/j.bmcl.2016.01.051. Epub 2016 Jan 19.

18.

Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.

Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17.

PMID:
26531152
19.

Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.

Kubas H, Meyer U, Hechenberger M, Klein KU, Plitt P, Zemribo R, Spexgoor HW, van Assema SG, Abel U.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6370-6. doi: 10.1016/j.bmcl.2013.09.059. Epub 2013 Sep 29.

PMID:
24125886
20.

Relationship between in vivo receptor occupancy and efficacy of metabotropic glutamate receptor subtype 5 allosteric modulators with different in vitro binding profiles.

Rook JM, Tantawy MN, Ansari MS, Felts AS, Stauffer SR, Emmitte KA, Kessler RM, Niswender CM, Daniels JS, Jones CK, Lindsley CW, Conn PJ.

Neuropsychopharmacology. 2015 Feb;40(3):755-65. doi: 10.1038/npp.2014.245. Epub 2014 Sep 22.

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