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Items: 44

1.

Target Engagement of a Phosphodiesterase 2A Inhibitor Affecting Long-Term Memory in the Rat.

Gu G, Scott T, Yan Y, Warren N, Zhang A, Tabatabaei A, Xu H, Aertgeerts K, Gomez L, Morse A, Li YW, Breitenbucher JG, Massari E, Vivian J, Danks A.

J Pharmacol Exp Ther. 2019 Sep;370(3):399-407. doi: 10.1124/jpet.118.255851. Epub 2019 Jun 28.

PMID:
31253692
2.

Mathematical and Structural Characterization of Strong Nonadditive Structure-Activity Relationship Caused by Protein Conformational Changes.

Gomez L, Xu R, Sinko W, Selfridge B, Vernier W, Ly K, Truong R, Metz M, Marrone T, Sebring K, Yan Y, Appleton B, Aertgeerts K, Massari ME, Breitenbucher JG.

J Med Chem. 2018 Sep 13;61(17):7754-7766. doi: 10.1021/acs.jmedchem.8b00713. Epub 2018 Aug 20.

PMID:
30070482
3.

Design and Synthesis of Novel and Selective Glycine Transporter-1 (GlyT1) Inhibitors with Memory Enhancing Properties.

Santora VJ, Almos TA, Barido R, Basinger J, Bellows CL, Bookser BC, Breitenbucher JG, Broadbent NJ, Cabebe C, Chai CK, Chen M, Chow S, Chung M, Crickard L, Danks AM, Freestone GC, Gitnick D, Gupta V, Hoffmaster C, Hudson AR, Kaplan AP, Kennedy MR, Lee D, Limberis J, Ly K, Mak CC, Masatsugu B, Morse AC, Na J, Neul D, Nikpur J, Peters M, Petroski RE, Renick J, Sebring K, Sevidal S, Tabatabaei A, Wen J, Yan Y, Yoder ZW, Zook D.

J Med Chem. 2018 Jul 26;61(14):6018-6033. doi: 10.1021/acs.jmedchem.8b00372. Epub 2018 Jul 11.

PMID:
29886732
4.

Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.

Dyck B, Branstetter B, Gharbaoui T, Hudson AR, Breitenbucher JG, Gomez L, Botrous I, Marrone T, Barido R, Allerston CK, Cedervall EP, Xu R, Sridhar V, Barker R, Aertgeerts K, Schmelzer K, Neul D, Lee D, Massari ME, Andersen CB, Sebring K, Zhou X, Petroski R, Limberis J, Augustin M, Chun LE, Edwards TE, Peters M, Tabatabaei A.

J Med Chem. 2017 Apr 27;60(8):3472-3483. doi: 10.1021/acs.jmedchem.7b00302. Epub 2017 Apr 13.

PMID:
28406621
5.

Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.

Gomez L, Massari ME, Vickers T, Freestone G, Vernier W, Ly K, Xu R, McCarrick M, Marrone T, Metz M, Yan YG, Yoder ZW, Lemus R, Broadbent NJ, Barido R, Warren N, Schmelzer K, Neul D, Lee D, Andersen CB, Sebring K, Aertgeerts K, Zhou X, Tabatabaei A, Peters M, Breitenbucher JG.

J Med Chem. 2017 Mar 9;60(5):2037-2051. doi: 10.1021/acs.jmedchem.6b01793. Epub 2017 Feb 21.

PMID:
28165743
6.

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.

Rech JC, Bhattacharya A, Branstetter BJ, Love CJ, Leenaerts JE, Cooymans LP, Eckert WA 3rd, Ao H, Wang Q, Chaplan SR, Wickenden AD, Lebsack AD, Breitenbucher JG.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4781-4784. doi: 10.1016/j.bmcl.2016.08.029. Epub 2016 Aug 20.

PMID:
27595421
7.

The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.

Keith JM, Tichenor MS, Apodaca RL, Xiao W, Jones WM, Seierstad M, Pierce JM, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Wennerholm ML, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3109-3114. doi: 10.1016/j.bmcl.2016.05.001. Epub 2016 May 5.

PMID:
27189675
8.

Preclinical Characterization of the FAAH Inhibitor JNJ-42165279.

Keith JM, Jones WM, Tichenor M, Liu J, Seierstad M, Palmer JA, Webb M, Karbarz M, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG.

ACS Med Chem Lett. 2015 Nov 2;6(12):1204-8. doi: 10.1021/acsmedchemlett.5b00353. eCollection 2015 Dec 10.

9.

1-Aryl-2-((6-aryl)pyrimidin-4-yl)amino)ethanols as competitive inhibitors of fatty acid amide hydrolase.

Keith JM, Hawryluk N, Apodaca RL, Chambers A, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Rizzolio M, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1280-4. doi: 10.1016/j.bmcl.2014.01.064. Epub 2014 Jan 31.

PMID:
24513048
10.

Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.

Keith JM, Jones WM, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Brown SM, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):737-41. doi: 10.1016/j.bmcl.2013.12.113. Epub 2014 Jan 6.

PMID:
24433863
11.

PDE2 inhibition: potential for the treatment of cognitive disorders.

Gomez L, Breitenbucher JG.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6522-7. doi: 10.1016/j.bmcl.2013.10.014. Epub 2013 Oct 24. Review.

12.

Heteroaryl urea inhibitors of fatty acid amide hydrolase: structure-mutagenicity relationships for arylamine metabolites.

Tichenor MS, Keith JM, Jones WM, Pierce JM, Merit J, Hawryluk N, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Wilson SJ, Wennerholm ML, Woestenborghs F, Beerens D, Luo L, Brown SM, Boeck MD, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7357-62. doi: 10.1016/j.bmcl.2012.10.076. Epub 2012 Oct 22.

PMID:
23141911
13.

Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.

Keith JM, Apodaca R, Tichenor M, Xiao W, Jones W, Pierce J, Seierstad M, Palmer J, Webb M, Karbarz M, Scott B, Wilson S, Luo L, Wennerholm M, Chang L, Brown S, Rizzolio M, Rynberg R, Chaplan S, Breitenbucher JG.

ACS Med Chem Lett. 2012 Aug 22;3(10):823-7. doi: 10.1021/ml300186g. eCollection 2012 Oct 11.

14.

Discovery of a novel series of selective HCN1 blockers.

McClure KJ, Maher M, Wu N, Chaplan SR, Eckert WA 3rd, Lee DH, Wickenden AD, Hermann M, Allison B, Hawryluk N, Breitenbucher JG, Grice CA.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5197-201. doi: 10.1016/j.bmcl.2011.07.051. Epub 2011 Jul 23.

PMID:
21824780
15.

Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.

Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR.

Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10.

PMID:
21575625
16.

Practical and scalable synthesis of a selective CCK1 receptor antagonist.

Mapes CM, Mani NS, Deng X, Pandit CR, McClure KJ, Pippel MC, Sehon CA, Gomez L, Shinde S, Breitenbucher JG, Jones TK.

J Org Chem. 2010 Nov 19;75(22):7950-3. doi: 10.1021/jo1017684. Epub 2010 Oct 27.

PMID:
20977279
17.

Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.

Hawryluk NA, Merit JE, Lebsack AD, Branstetter BJ, Hack MD, Swanson N, Ao H, Maher MP, Bhattacharya A, Wang Q, Freedman JM, Scott BP, Wickenden AD, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7137-41. doi: 10.1016/j.bmcl.2010.09.023. Epub 2010 Sep 17.

PMID:
20947352
18.

1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.

Lebsack AD, Rech JC, Branstetter BJ, Hawryluk NA, Merit JE, Allison B, Rynberg R, Buma J, Rizzolio M, Swanson N, Ao H, Maher MP, Herrmann M, Freedman J, Scott BP, Luo L, Bhattacharya A, Wang Q, Chaplan SR, Wickenden AD, Breitenbucher JG.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):7142-6. doi: 10.1016/j.bmcl.2010.09.006. Epub 2010 Sep 7.

PMID:
20932750
19.

Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase.

Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M.

Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd.

PMID:
19095868
20.

Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.

Seierstad M, Breitenbucher JG.

J Med Chem. 2008 Dec 11;51(23):7327-43. doi: 10.1021/jm800311k. Review. No abstract available.

PMID:
18983142
21.

Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase.

Keith JM, Apodaca R, Xiao W, Seierstad M, Pattabiraman K, Wu J, Webb M, Karbarz MJ, Brown S, Wilson S, Scott B, Tham CS, Luo L, Palmer J, Wennerholm M, Chaplan S, Breitenbucher JG.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43. doi: 10.1016/j.bmcl.2008.07.081. Epub 2008 Jul 25.

PMID:
18693015
22.

Role of CCK and potential utility of CCK1 receptor antagonism in the treatment of pancreatitis induced by biliary tract obstruction.

Barrett TD, Yan W, Freedman JM, Lagaud GJ, Breitenbucher JG, Shankley NP.

Br J Pharmacol. 2008 Apr;153(8):1650-8. doi: 10.1038/bjp.2008.44. Epub 2008 Feb 25.

23.

Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).

Timmons A, Seierstad M, Apodaca R, Epperson M, Pippel D, Brown S, Chang L, Scott B, Webb M, Chaplan SR, Breitenbucher JG.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2109-13. doi: 10.1016/j.bmcl.2008.01.091. Epub 2008 Jan 30.

PMID:
18289847
24.

Activation of TRPA1 by farnesyl thiosalicylic acid.

Maher M, Ao H, Banke T, Nasser N, Wu NT, Breitenbucher JG, Chaplan SR, Wickenden AD.

Mol Pharmacol. 2008 Apr;73(4):1225-34. doi: 10.1124/mol.107.042663. Epub 2008 Jan 2.

PMID:
18171730
25.

2-Aryl benzimidazoles featuring alkyl-linked pendant alcohols and amines as inhibitors of checkpoint kinase Chk2.

Neff DK, Lee-Dutra A, Blevitt JM, Axe FU, Hack MD, Buma JC, Rynberg R, Brunmark A, Karlsson L, Breitenbucher JG.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6467-71. Epub 2007 Oct 4.

PMID:
17937984
26.

SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.

Gomez L, Hack MD, McClure K, Sehon C, Huang L, Morton M, Li L, Barrett TD, Shankley N, Breitenbucher JG.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6493-8. Epub 2007 Oct 1.

PMID:
17933530
27.

3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.

Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP.

J Pharmacol Exp Ther. 2007 Nov;323(2):562-9. Epub 2007 Aug 7.

PMID:
17684117
28.

Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.

Romero FA, Du W, Hwang I, Rayl TJ, Kimball FS, Leung D, Hoover HS, Apodaca RL, Breitenbucher JG, Cravatt BF, Boger DL.

J Med Chem. 2007 Mar 8;50(5):1058-68. Epub 2007 Feb 6.

29.

Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.

Lee-Dutra A, Arienti KL, Buzard DJ, Hack MD, Khatuya H, Desai PJ, Nguyen S, Thurmond RL, Karlsson L, Edwards JP, Breitenbucher JG.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6043-8. Epub 2006 Sep 20.

PMID:
16990005
30.

Inhibition of fatty acid amide hydrolase produces analgesia by multiple mechanisms.

Chang L, Luo L, Palmer JA, Sutton S, Wilson SJ, Barbier AJ, Breitenbucher JG, Chaplan SR, Webb M.

Br J Pharmacol. 2006 May;148(1):102-13. Erratum in: Br J Pharmacol. 2006 May;148(1):114.

31.

Novel non-benzimidazole chk2 kinase inhibitors.

McClure KJ, Huang L, Arienti KL, Axe FU, Brunmark A, Blevitt J, Breitenbucher JG.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1924-8. Epub 2006 Jan 25.

PMID:
16442290
32.

Pyrazole CCK(1) receptor antagonists. Part 1: Solution-phase library synthesis and determination of Free-Wilson additivity.

McClure K, Hack M, Huang L, Sehon C, Morton M, Li L, Barrett TD, Shankley N, Breitenbucher JG.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):72-6. Epub 2005 Oct 19.

PMID:
16236513
33.

Pyrazole CCK(1) receptor antagonists. Part 2: SAR studies by solid-phase library synthesis and determination of Free-Wilson additivity.

Sehon C, McClure K, Hack M, Morton M, Gomez L, Li L, Barrett TD, Shankley N, Breitenbucher JG.

Bioorg Med Chem Lett. 2006 Jan 1;16(1):77-80. Epub 2005 Oct 19.

PMID:
16236506
34.

Checkpoint kinase inhibitors: SAR and radioprotective properties of a series of 2-arylbenzimidazoles.

Arienti KL, Brunmark A, Axe FU, McClure K, Lee A, Blevitt J, Neff DK, Huang L, Crawford S, Pandit CR, Karlsson L, Breitenbucher JG.

J Med Chem. 2005 Mar 24;48(6):1873-85.

PMID:
15771432
35.

Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.

Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI.

J Med Chem. 2005 Mar 24;48(6):1857-72.

PMID:
15771431
36.

Dihydropyridine neuropeptide Y Y1 receptor antagonists 2. bioisosteric urea replacements.

Poindexter GS, Bruce MA, Breitenbucher JG, Higgins MA, Sit SY, Romine JL, Martin SW, Ward SA, McGovern RT, Clarke W, Russell J, Antal-Zimanyi I.

Bioorg Med Chem. 2004 Jan 15;12(2):507-21.

PMID:
14723969
37.

The impact of combinatorial chemistry on drug discovery.

Lee A, Breitenbucher JG.

Curr Opin Drug Discov Devel. 2003 Jul;6(4):494-508. Review.

PMID:
12951813
38.

Elaborate manifold of short hydrogen bond arrays mediating binding of active site-directed serine protease inhibitors.

Katz BA, Elrod K, Verner E, Mackman RL, Luong C, Shrader WD, Sendzik M, Spencer JR, Sprengeler PA, Kolesnikov A, Tai VW, Hui HC, Breitenbucher JG, Allen D, Janc JW.

J Mol Biol. 2003 May 23;329(1):93-120.

PMID:
12742021
39.

Non-imidazole heterocyclic histamine H3 receptor antagonists.

Chai W, Breitenbucher JG, Kwok A, Li X, Wong V, Carruthers NI, Lovenberg TW, Mazur C, Wilson SJ, Axe FU, Jones TK.

Bioorg Med Chem Lett. 2003 May 19;13(10):1767-70.

PMID:
12729661
40.

Novel human histamine H(3) receptor antagonists.

Shah C, McAtee L, Breitenbucher JG, Rudolph D, Li X, Lovenberg TW, Mazur C, Wilson SJ, Carruthers NI.

Bioorg Med Chem Lett. 2002 Nov 18;12(22):3309-12.

PMID:
12392739
41.

2-(2-Hydroxy-3-alkoxyphenyl)-1H-benzimidazole-5-carboxamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.

Mackman RL, Hui HC, Breitenbucher JG, Katz BA, Luong C, Martelli A, McGee D, Radika K, Sendzik M, Spencer JR, Sprengeler PA, Tario J, Verner E, Wang J.

Bioorg Med Chem Lett. 2002 Aug 5;12(15):2019-22.

PMID:
12113832
42.

Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets.

Katz BA, Sprengeler PA, Luong C, Verner E, Elrod K, Kirtley M, Janc J, Spencer JR, Breitenbucher JG, Hui H, McGee D, Allen D, Martelli A, Mackman RL.

Chem Biol. 2001 Nov;8(11):1107-21.

43.

Scope and limitations of solid-supported liquid-liquid extraction for the high-throughput purification of compound libraries.

Breitenbucher JG, Arienti KL, McClure KJ.

J Comb Chem. 2001 Nov-Dec;3(6):528-33.

PMID:
11703147
44.

Exploiting subsite S1 of trypsin-like serine proteases for selectivity: potent and selective inhibitors of urokinase-type plasminogen activator.

Mackman RL, Katz BA, Breitenbucher JG, Hui HC, Verner E, Luong C, Liu L, Sprengeler PA.

J Med Chem. 2001 Nov 8;44(23):3856-71.

PMID:
11689072

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