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Items: 1 to 50 of 152

1.

Increased stress associated with head-out plethysmography testing can exacerbate respiratory effects and lead to mortality in rats.

Lynch JJ 3rd, Rossignol E, Moehrle JJ, Van Vleet TR, Marsh KC, Parman T, Mirsalis J, Ottinger SE, Segreti JA, Rao M, Mittelstadt SW.

J Pharmacol Toxicol Methods. 2019 May 11:106580. doi: 10.1016/j.vascn.2019.106580. [Epub ahead of print]

PMID:
31085318
2.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

3.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

4.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

5.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain.

Beebe X, Yeung CM, Darczak D, Shekhar S, Vortherms TA, Miller L, Milicic I, Swensen AM, Zhu CZ, Banfor P, Wetter JM, Marsh KC, Jarvis MF, Scott VE, Schrimpf MR, Lee CH.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4857-61. doi: 10.1016/j.bmcl.2013.06.074. Epub 2013 Jul 4.

PMID:
23876987
6.

Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A.

DeGoey DA, Betebenner DA, Grampovnik DJ, Liu D, Pratt JK, Tufano MD, He W, Krishnan P, Pilot-Matias TJ, Marsh KC, Molla A, Kempf DJ, Maring CJ.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3627-30. doi: 10.1016/j.bmcl.2013.04.009. Epub 2013 Apr 10.

PMID:
23642966
7.

Species-dependent metabolism of a novel selective α7 neuronal acetylcholine receptor agonist ABT-107.

Liu H, Deng X, Liu J, Liu N, Stuart P, Xu H, Guan Z, Marsh KC, De Morais SM.

Xenobiotica. 2013 Sep;43(9):803-16. doi: 10.3109/00498254.2012.760763. Epub 2013 Jan 18.

PMID:
23327533
8.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.

Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW.

Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6.

PMID:
23291630
9.

AhR activation underlies the CYP1A autoinduction by A-998679 in rats.

Liguori MJ, Lee CH, Liu H, Ciurlionis R, Ditewig AC, Doktor S, Andracki ME, Gagne GD, Waring JF, Marsh KC, Gopalakrishnan M, Blomme EA, Yang Y.

Front Genet. 2012 Oct 26;3:213. doi: 10.3389/fgene.2012.00213. eCollection 2012.

10.

Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity.

Beebe X, Darczak D, Henry RF, Vortherms T, Janis R, Namovic M, Donnelly-Roberts D, Kage KL, Surowy C, Milicic I, Niforatos W, Swensen A, Marsh KC, Wetter JM, Franklin P, Baker S, Zhong C, Simler G, Gomez E, Boyce-Rustay JM, Zhu CZ, Stewart AO, Jarvis MF, Scott VE.

Bioorg Med Chem. 2012 Jul 1;20(13):4128-39. doi: 10.1016/j.bmc.2012.04.057. Epub 2012 May 4.

PMID:
22626552
11.

Discovery of diphenyl lactam derivatives as N-type calcium channel blockers.

Doherty GA, Bhatia P, Vortherms TA, Marsh KC, Wetter JM, Mack H, Scott VE, Jarvis MF, Stewart AO.

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1716-8. doi: 10.1016/j.bmcl.2011.12.100. Epub 2012 Jan 8.

PMID:
22277280
12.

Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.

Yeh VS, Beno DW, Brodjian S, Brune ME, Cullen SC, Dayton BD, Dhaon MK, Falls HD, Gao J, Grihalde N, Hajduk P, Hansen TM, Judd AS, King AJ, Klix RC, Larson KJ, Lau YY, Marsh KC, Mittelstadt SW, Plata D, Rozema MJ, Segreti JA, Stoner EJ, Voorbach MJ, Wang X, Xin X, Zhao G, Collins CA, Cox BF, Reilly RM, Kym PR, Souers AJ.

J Med Chem. 2012 Feb 23;55(4):1751-7. doi: 10.1021/jm201524g. Epub 2012 Feb 10.

PMID:
22263872
13.

N-vinylpyrrolidone dimer, a novel formulation excipient, causes hepatic and thyroid hypertrophy through the induction of hepatic microsomal enzymes in rats.

Yang Y, Ciurlionis R, Kowalkowski K, Marsh KC, Bracken WM, Blomme EA.

Toxicol Lett. 2012 Jan 5;208(1):82-91. doi: 10.1016/j.toxlet.2011.10.012. Epub 2011 Oct 20.

PMID:
22037397
14.

Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.

Scanio MJ, Shi L, Bunnelle WH, Anderson DJ, Helfrich RJ, Malysz J, Thorin-Hagene KK, Van Handel CE, Marsh KC, Lee CH, Gopalakrishnan M.

J Med Chem. 2011 Nov 10;54(21):7678-92. doi: 10.1021/jm201045m. Epub 2011 Oct 11.

PMID:
21962147
15.

Role of α7 nicotinic acetylcholine receptors in regulating tumor necrosis factor-α (TNF-α) as revealed by subtype selective agonists.

Li J, Mathieu SL, Harris R, Ji J, Anderson DJ, Malysz J, Bunnelle WH, Waring JF, Marsh KC, Murtaza A, Olson LM, Gopalakrishnan M.

J Neuroimmunol. 2011 Oct 28;239(1-2):37-43. doi: 10.1016/j.jneuroim.2011.08.007. Epub 2011 Sep 10.

PMID:
21911260
16.

Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.

Schmidt RG, Bayburt EK, Latshaw SP, Koenig JR, Daanen JF, McDonald HA, Bianchi BR, Zhong C, Joshi S, Honore P, Marsh KC, Lee CH, Faltynek CR, Gomtsyan A.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1338-41. doi: 10.1016/j.bmcl.2011.01.056. Epub 2011 Jan 21.

PMID:
21315587
17.

Pharmacokinetic modeling and [¹²³]5-IA-85380 single photon emission computed tomography imaging in baboons: optimization of dosing regimen for ABT-089.

Chin CL, Carr RA, Llano DA, Barret O, Xu H, Batis J, Koren AO, Seibyl JP, Marsh KC, Tamagnan G, Decker MW, Day M, Fox GB.

J Pharmacol Exp Ther. 2011 Mar;336(3):716-23. doi: 10.1124/jpet.110.173609. Epub 2010 Dec 20.

PMID:
21172907
18.

Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.

Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME.

Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29.

PMID:
20965738
19.

Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain.

Altenbach RJ, Black LA, Strakhova MI, Manelli AM, Carr TL, Marsh KC, Wetter JM, Wensink EJ, Hsieh GC, Honore P, Garrison TR, Brioni JD, Cowart MD.

J Med Chem. 2010 Nov 11;53(21):7869-73. doi: 10.1021/jm100666w.

PMID:
20945906
20.

Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.

Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18.

PMID:
20855211
21.

Liver transcriptomic changes associated with ritonavir-induced hyperlipidemia in sensitive and resistant strains of rats.

Yang Y, Dahly-Vernon AJ, Blomme EA, Lai-Zhang J, Kempf DJ, Marsh KC, Harrington YA, Nye SH, Evans DL, Roman RJ, Jacob HJ, Waring JF.

Vet J. 2010 Jul;185(1):75-82. doi: 10.1016/j.tvjl.2010.04.017. Epub 2010 May 23.

PMID:
20547082
22.

In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease.

Bitner RS, Bunnelle WH, Decker MW, Drescher KU, Kohlhaas KL, Markosyan S, Marsh KC, Nikkel AL, Browman K, Radek R, Anderson DJ, Buccafusco J, Gopalakrishnan M.

J Pharmacol Exp Ther. 2010 Sep 1;334(3):875-86. doi: 10.1124/jpet.110.167213. Epub 2010 May 26.

PMID:
20504913
23.

Discovery of TRPV1 antagonist ABT-116.

Brown BS, Keddy R, Perner RJ, DiDomenico S, Koenig JR, Jinkerson TK, Hannick SM, McDonald HA, Bianchi BR, Honore P, Puttfarcken PS, Moreland RB, Marsh KC, Faltynek CR, Lee CH.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3291-4. doi: 10.1016/j.bmcl.2010.04.047. Epub 2010 Apr 14.

PMID:
20457518
24.

Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.

Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.

J Med Chem. 2010 Apr 22;53(8):3142-53. doi: 10.1021/jm901775y.

PMID:
20337371
25.

Tumour-selective antivascular effects of the novel anti-mitotic compound A-318315: An in vivo rat regional haemodynamic study.

Segreti JA, Brooks KA, Marsh KC, Bauch JL, Lan Y, Thomas Lin C, Rosenberg SH, Sham HL, Reinhart GA, Cox BF, Polakowski JS.

Clin Exp Pharmacol Physiol. 2010 May;37(5-6):636-40. doi: 10.1111/j.1440-1681.2010.05365.x. Epub 2010 Feb 4.

PMID:
20132238
26.

H4 receptor antagonism exhibits anti-nociceptive effects in inflammatory and neuropathic pain models in rats.

Hsieh GC, Chandran P, Salyers AK, Pai M, Zhu CZ, Wensink EJ, Witte DG, Miller TR, Mikusa JP, Baker SJ, Wetter JM, Marsh KC, Hancock AA, Cowart MD, Esbenshade TA, Brioni JD, Honore P.

Pharmacol Biochem Behav. 2010 Mar;95(1):41-50. doi: 10.1016/j.pbb.2009.12.004. Epub 2009 Dec 11.

PMID:
20004681
27.

Cardiovascular effects of torcetrapib in conscious and pentobarbital-anesthetized dogs.

Polakowski JS, King AJ, Campbell TJ, Nelson RA, Preusser LC, Kempf-Grote AJ, Marsh KC, Gintant GA, Cox BF, Mittelstadt SW.

J Cardiovasc Pharmacol. 2009 Dec;54(6):543-51. doi: 10.1097/FJC.0b013e3181bfb158.

PMID:
19770671
28.

Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.

Flentge CA, Randolph JT, Huang PP, Klein LL, Marsh KC, Harlan JE, Kempf DJ.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5444-8. doi: 10.1016/j.bmcl.2009.07.118. Epub 2009 Jul 30.

PMID:
19679477
29.

Design of a new histamine H3 receptor antagonist chemotype: (3aR,6aR)-5-alkyl-1-aryl-octahydropyrrolo[3,4-b]pyrroles, synthesis, and structure-activity relationships.

Zhao C, Sun M, Bennani YL, Miller TR, Witte DG, Esbenshade TA, Wetter J, Marsh KC, Hancock AA, Brioni JD, Cowart MD.

J Med Chem. 2009 Aug 13;52(15):4640-9. doi: 10.1021/jm900480x.

PMID:
19588934
30.

Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.

Faghih R, Gopalakrishnan SM, Gronlien JH, Malysz J, Briggs CA, Wetterstrand C, Ween H, Curtis MP, Sarris KA, Gfesser GA, El-Kouhen R, Robb HM, Radek RJ, Marsh KC, Bunnelle WH, Gopalakrishnan M.

J Med Chem. 2009 May 28;52(10):3377-84. doi: 10.1021/jm9003818.

PMID:
19419141
31.

In vitro and in vivo characterization of A-940894: a potent histamine H4 receptor antagonist with anti-inflammatory properties.

Strakhova MI, Cuff CA, Manelli AM, Carr TL, Witte DG, Baranowski JL, Vortherms TA, Miller TR, Rundell L, McPherson MJ, Adair RM, Brito AA, Bettencourt BM, Yao BB, Wetter JM, Marsh KC, Liu H, Cowart MD, Brioni JD, Esbenshade TA.

Br J Pharmacol. 2009 May;157(1):44-54. doi: 10.1111/j.1476-5381.2009.00236.x.

32.

Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.

DeGoey DA, Grampovnik DJ, Flosi WJ, Marsh KC, Wang XC, Klein LL, McDaniel KF, Liu Y, Long MA, Kati WM, Molla A, Kempf DJ.

J Med Chem. 2009 May 14;52(9):2964-70. doi: 10.1021/jm900080g.

PMID:
19348416
33.

2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.

Degoey DA, Grampovnik DJ, Flentge CA, Flosi WJ, Chen HJ, Yeung CM, Randolph JT, Klein LL, Dekhtyar T, Colletti L, Marsh KC, Stoll V, Mamo M, Morfitt DC, Nguyen B, Schmidt JM, Swanson SJ, Mo H, Kati WM, Molla A, Kempf DJ.

J Med Chem. 2009 Apr 23;52(8):2571-86. doi: 10.1021/jm900044w.

PMID:
19323562
34.

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.

Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.

J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j.

PMID:
19143569
35.

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.

J Med Chem. 2008 Nov 27;51(22):7094-8. doi: 10.1021/jm8007618.

PMID:
18983139
36.

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

Park CM, Bruncko M, Adickes J, Bauch J, Ding H, Kunzer A, Marsh KC, Nimmer P, Shoemaker AR, Song X, Tahir SK, Tse C, Wang X, Wendt MD, Yang X, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.

J Med Chem. 2008 Nov 13;51(21):6902-15. doi: 10.1021/jm800669s. Epub 2008 Oct 8.

PMID:
18841882
37.

Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.

Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, Miller TR, Witte DG, Wishart N, Fix-Stenzel SR, McPherson MJ, Adair RM, Wetter JM, Bettencourt BM, Marsh KC, Sullivan JP, Honore P, Esbenshade TA, Brioni JD.

J Med Chem. 2008 Oct 23;51(20):6547-57. doi: 10.1021/jm800670r. Epub 2008 Sep 26.

PMID:
18817367
38.

Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.

Altenbach RJ, Adair RM, Bettencourt BM, Black LA, Fix-Stenzel SR, Gopalakrishnan SM, Hsieh GC, Liu H, Marsh KC, McPherson MJ, Milicic I, Miller TR, Vortherms TA, Warrior U, Wetter JM, Wishart N, Witte DG, Honore P, Esbenshade TA, Hancock AA, Brioni JD, Cowart MD.

J Med Chem. 2008 Oct 23;51(20):6571-80. doi: 10.1021/jm8005959. Epub 2008 Sep 24.

PMID:
18811133
39.

Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.

Brown BS, Keddy R, Zheng GZ, Schmidt RG, Koenig JR, McDonald HA, Bianchi BR, Honore P, Jarvis MF, Surowy CS, Polakowski JS, Marsh KC, Faltynek CR, Lee CH.

Bioorg Med Chem. 2008 Sep 15;16(18):8516-25. doi: 10.1016/j.bmc.2008.08.005. Epub 2008 Aug 7.

PMID:
18722778
40.

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.

Zhao C, Sun M, Bennani YL, Gopalakrishnan SM, Witte DG, Miller TR, Krueger KM, Browman KE, Thiffault C, Wetter J, Marsh KC, Hancock AA, Esbenshade TA, Cowart MD.

J Med Chem. 2008 Sep 11;51(17):5423-30. doi: 10.1021/jm8003625. Epub 2008 Aug 7.

PMID:
18683917
41.

Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.

Zhu GD, Gandhi VB, Gong J, Thomas S, Luo Y, Liu X, Shi Y, Klinghofer V, Johnson EF, Frost D, Donawho C, Jarvis K, Bouska J, Marsh KC, Rosenberg SH, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3955-8. doi: 10.1016/j.bmcl.2008.06.023. Epub 2008 Jun 12.

PMID:
18586490
42.

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.

Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL.

Bioorg Med Chem. 2008 Jul 15;16(14):6965-75. doi: 10.1016/j.bmc.2008.05.044. Epub 2008 May 27.

PMID:
18541433
43.

Dose-response effects of sotalol on cardiovascular function in conscious, freely moving cynomolgus monkeys.

Lynch JJ 3rd, Wilson AW, Hernandez LE, Nelson RA, Marsh KC, Cox BF, Mittelstadt SW.

Br J Pharmacol. 2008 Aug;154(7):1439-45. doi: 10.1038/bjp.2008.206. Epub 2008 Jun 2.

44.

Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.

Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Thomas JB, Johnson MS, Carroll WA, Marron BE, Chapman ML, Liu D, Krambis MJ, Shieh CC, Zhang X, Hernandez G, Gauvin DM, Mikusa JP, Zhu CZ, Joshi S, Honore P, Marsh KC, Roeloffs R, Werness S, Krafte DS, Jarvis MF, Faltynek CR, Kort ME.

Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. doi: 10.1016/j.bmc.2008.05.003. Epub 2008 May 6.

PMID:
18501613
45.

Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties.

Tietje KR, Anderson DJ, Bitner RS, Blomme EA, Brackemeyer PJ, Briggs CA, Browman KE, Bury D, Curzon P, Drescher KU, Frost JM, Fryer RM, Fox GB, Gronlien JH, Håkerud M, Gubbins EJ, Halm S, Harris R, Helfrich RJ, Kohlhaas KL, Law D, Malysz J, Marsh KC, Martin RL, Meyer MD, Molesky AL, Nikkel AL, Otte S, Pan L, Puttfarcken PS, Radek RJ, Robb HM, Spies E, Thorin-Hagene K, Waring JF, Ween H, Xu H, Gopalakrishnan M, Bunnelle WH.

CNS Neurosci Ther. 2008 Spring;14(1):65-82. doi: 10.1111/j.1527-3458.2008.00037.x. Review.

PMID:
18482100
46.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

Tse C, Shoemaker AR, Adickes J, Anderson MG, Chen J, Jin S, Johnson EF, Marsh KC, Mitten MJ, Nimmer P, Roberts L, Tahir SK, Xiao Y, Yang X, Zhang H, Fesik S, Rosenberg SH, Elmore SW.

Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836.

47.

Minimization of potential hERG liability in histamine H3 receptor antagonists.

Black LA, Liu H, Diaz GJ, Fox GB, Browman KE, Wetter J, Marsh KC, Miller TR, Esbenshade TA, Brioni J, Cowart MD.

Inflamm Res. 2008;57 Suppl 1:S45-6. doi: 10.1007/s00011-007-0622-2. No abstract available.

PMID:
18345496
48.

Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.

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Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.

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Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.

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J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5.

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