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Items: 1 to 50 of 71

1.

Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Panarese JD, Engers DW, Wu YJ, Bronson JJ, Macor JE, Chun A, Rodriguez AL, Felts AS, Engers JL, Loch MT, Emmitte KA, Castelhano AL, Kates MJ, Nader MA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

ACS Med Chem Lett. 2018 Oct 16;10(3):255-260. doi: 10.1021/acsmedchemlett.8b00426. eCollection 2019 Mar 14.

PMID:
30891122
2.

The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.

Panarese JD, Engers DW, Wu YJ, Guernon JM, Chun A, Gregro AR, Bender AM, Capstick RA, Wieting JM, Bronson JJ, Macor JE, Westphal R, Soars M, Engers JE, Felts AS, Rodriguez AL, Emmitte KA, Jones CK, Blobaum AL, Conn PJ, Niswender CM, Hopkins CR, Lindsley CW.

Bioorg Med Chem Lett. 2019 Jan 15;29(2):342-346. doi: 10.1016/j.bmcl.2018.10.050. Epub 2018 Nov 1.

PMID:
30503632
3.

Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.

Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2018 Aug 15;28(15):2641-2646. doi: 10.1016/j.bmcl.2018.06.034. Epub 2018 Jun 19.

PMID:
29958762
4.

BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.

Marcin LR, Warrier J, Thangathirupathy S, Shi J, Karageorge GN, Pearce BC, Ng A, Park H, Kempson J, Li J, Zhang H, Mathur A, Reddy AB, Nagaraju G, Tonukunuru G, Gupta GVRKM, Kamble M, Mannoori R, Cheruku S, Jogi S, Gulia J, Bastia T, Sanmathi C, Aher J, Kallem R, Srikumar BN, Vijaya KK, Naidu PS, Paschapur M, Kalidindi N, Vikramadithyan R, Ramarao M, Denton R, Molski T, Shields E, Subramanian M, Zhuo X, Nophsker M, Simmermacher J, Sinz M, Albright C, Bristow LJ, Islam I, Bronson JJ, Olson RE, King D, Thompson LA, Macor JE.

ACS Med Chem Lett. 2018 Apr 13;9(5):472-477. doi: 10.1021/acsmedchemlett.8b00080. eCollection 2018 May 10.

5.

Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.

Bristow LJ, Gulia J, Weed MR, Srikumar BN, Li YW, Graef JD, Naidu PS, Sanmathi C, Aher J, Bastia T, Paschapur M, Kalidindi N, Kumar KV, Molski T, Pieschl R, Fernandes A, Brown JM, Sivarao DV, Newberry K, Bookbinder M, Polino J, Keavy D, Newton A, Shields E, Simmermacher J, Kempson J, Li J, Zhang H, Mathur A, Kallem RR, Sinha M, Ramarao M, Vikramadithyan RK, Thangathirupathy S, Warrier J, Islam I, Bronson JJ, Olson RE, Macor JE, Albright CF, King D, Thompson LA, Marcin LR, Sinz M.

J Pharmacol Exp Ther. 2017 Dec;363(3):377-393. doi: 10.1124/jpet.117.242784. Epub 2017 Sep 27.

PMID:
28954811
6.

Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability.

Hartz RA, Vrudhula VM, Ahuja VT, Grace JE, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1360-1363. doi: 10.1016/j.bmcl.2017.02.015. Epub 2017 Feb 10.

PMID:
28223020
7.

Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.

Hill MD, Fang H, Brown JM, Molski T, Easton A, Han X, Miller R, Hill-Drzewi M, Gallagher L, Matchett M, Gulianello M, Balakrishnan A, Bertekap RL, Santone KS, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE, Degnan AP.

ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086. eCollection 2016 Dec 8.

8.

Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.

Higgins MA, Marcin LR, Christopher Zusi F, Gentles R, Ding M, Pearce BC, Easton A, Kostich WA, Seager MA, Bourin C, Bristow LJ, Johnson KA, Miller R, Hogan J, Whiterock V, Gulianello M, Ferrante M, Huang Y, Hendricson A, Alt A, Macor JE, Bronson JJ.

Bioorg Med Chem. 2017 Jan 15;25(2):496-513. doi: 10.1016/j.bmc.2016.11.018. Epub 2016 Nov 14.

PMID:
27914948
9.

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential.

Degnan AP, Maxwell D, Balakrishnan A, Brown JM, Easton A, Gulianello M, Hanumegowda U, Hill-Drzewi M, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Westphal R, Whiterock VJ, Zhuo X, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Dec 15;26(24):5871-5876. doi: 10.1016/j.bmcl.2016.11.014. Epub 2016 Nov 9.

PMID:
27856084
10.

Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.

Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW.

ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18.

PMID:
27744678
11.

Oxazolidinone-based allosteric modulators of mGluR5: Defining molecular switches to create a pharmacological tool box.

Huang H, Degnan AP, Balakrishnan A, Easton A, Gulianello M, Huang Y, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Sivarao DV, Snyder LB, Westphal R, Whiterock VJ, Yang F, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. doi: 10.1016/j.bmcl.2016.07.065. Epub 2016 Jul 28.

PMID:
27496211
12.

Discovery, Synthesis, and Preclinical Characterization of N-(3-Chloro-4-fluorophenyl)-1H-pyrazolo[4,3-b]pyridin-3-amine (VU0418506), a Novel Positive Allosteric Modulator of the Metabotropic Glutamate Receptor 4 (mGlu4).

Engers DW, Blobaum AL, Gogliotti RD, Cheung YY, Salovich JM, Garcia-Barrantes PM, Daniels JS, Morrison R, Jones CK, Soars MG, Zhuo X, Hurley J, Macor JE, Bronson JJ, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

ACS Chem Neurosci. 2016 Sep 21;7(9):1192-200. doi: 10.1021/acschemneuro.6b00035. Epub 2016 May 3.

13.

Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF₁) receptor antagonists.

Ahuja VT, Hartz RA, Molski TF, Mattson GK, Lentz KA, Grace JE Jr, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2016 May 1;26(9):2184-7. doi: 10.1016/j.bmcl.2016.03.067. Epub 2016 Mar 17.

PMID:
27020524
14.

Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5.

Yang F, Snyder LB, Balakrishnan A, Brown JM, Sivarao DV, Easton A, Fernandes A, Gulianello M, Hanumegowda UM, Huang H, Huang Y, Jones KM, Li YW, Matchett M, Mattson G, Miller R, Santone KS, Senapati A, Shields EE, Simutis FJ, Westphal R, Whiterock VJ, Bronson JJ, Macor JE, Degnan AP.

ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. doi: 10.1021/acsmedchemlett.5b00450. eCollection 2016 Mar 10.

15.

Biochemical and behavioral effects of PDE10A inhibitors: Relationship to target site occupancy.

Li YW, Seager MA, Wojcik T, Heman K, Molski TF, Fernandes A, Langdon S, Pendri A, Gerritz S, Tian Y, Hong Y, Gallagher L, Merritt JR, Zhang C, Westphal R, Zaczek R, Macor JE, Bronson JJ, Lodge NJ.

Neuropharmacology. 2016 Mar;102:121-35. doi: 10.1016/j.neuropharm.2015.10.037. Epub 2015 Oct 30.

PMID:
26522433
16.

Biaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors.

Degnan AP, Tora GO, Han Y, Rajamani R, Bertekap R, Krause R, Davis CD, Hu J, Morgan D, Taylor SJ, Krause K, Li YW, Mattson G, Cunningham MA, Taber MT, Lodge NJ, Bronson JJ, Gillman KW, Macor JE.

Bioorg Med Chem Lett. 2015 Aug 1;25(15):3039-43. doi: 10.1016/j.bmcl.2015.04.098. Epub 2015 Jun 2.

PMID:
26048800
17.

The discovery of potent agonists for GPR88, an orphan GPCR, for the potential treatment of CNS disorders.

Bi Y, Dzierba CD, Fink C, Garcia Y, Green M, Han J, Kwon S, Kumi G, Liang Z, Liu Y, Qiao Y, Zhang Y, Zipp G, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Westphal RS, Kimball D, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1443-7. doi: 10.1016/j.bmcl.2015.02.038. Epub 2015 Feb 21.

PMID:
25754495
18.

Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.

Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28.

PMID:
25690789
19.

Synthesis and evaluation of candidate PET radioligands for corticotropin-releasing factor type-1 receptors.

Lodge NJ, Li YW, Chin FT, Dischino DD, Zoghbi SS, Deskus JA, Mattson RJ, Imaizumi M, Pieschl R, Molski TF, Fujita M, Dulac H, Zaczek R, Bronson JJ, Macor JE, Innis RB, Pike VW.

Nucl Med Biol. 2014 Jul;41(6):524-35. doi: 10.1016/j.nucmedbio.2014.03.005. Epub 2014 Mar 29.

20.

NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.

Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ.

Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12.

PMID:
23770339
21.

Potential CRF1R PET imaging agents: 1-fluoroalkylsubstituted 5-halo-3-(arylamino)pyrazin-2(1H)-ones.

Denhart DJ, Zuev D, Ditta JL, Hartz RA, Ahuja VT, Mattson RJ, Huang H, Mattson GK, Zueva L, Nielsen JM, Kozlowski ES, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2052-5. doi: 10.1016/j.bmcl.2013.02.009. Epub 2013 Feb 13.

PMID:
23465610
22.

Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression.

Gillman KW, Parker MF, Silva M, Degnan AP, Tora GO, Lodge NJ, Li YW, Lelas S, Taber M, Krause RG, Bertekap RL, Newton AE, Pieschl RL, Lengyel KD, Johnson KA, Taylor SJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):407-11. doi: 10.1016/j.bmcl.2012.11.094. Epub 2012 Nov 30.

PMID:
23253443
23.

Pharmacological and behavioral characterization of the novel CRF1 antagonist BMS-763534.

Lodge NJ, Lelas S, Li YW, Molski T, Grace J, Sivarao DV, Post-Munson D, Healy F, Bronson JJ, Hartz R, Macor JE, Zaczek R.

Neuropharmacology. 2013 Apr;67:284-93. doi: 10.1016/j.neuropharm.2012.10.025. Epub 2012 Nov 19.

PMID:
23174340
24.

2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.

Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Dee MF, Gai Y, Guss VL, Higgins MA, Keavy DJ, Loo A, Mate RA, Marcin LR, McElhone KE, Polson CT, Roberts SB, Macor JE.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6828-31. doi: 10.1016/j.bmcl.2012.09.057. Epub 2012 Sep 24.

PMID:
23046960
25.

[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.

Deskus JA, Dischino DD, Mattson RJ, Ditta JL, Parker MF, Denhart DJ, Zuev D, Huang H, Hartz RA, Ahuja VT, Wong H, Mattson GK, Molski TF, Grace JE Jr, Zueva L, Nielsen JM, Dulac H, Li YW, Guaraldi M, Azure M, Onthank D, Hayes M, Wexler E, McDonald J, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Nov 1;22(21):6651-5. doi: 10.1016/j.bmcl.2012.08.112. Epub 2012 Sep 7.

PMID:
23010264
26.

Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.

Dzierba CD, Sielecki TM, Arvanitis AG, Galka A, Johnson TL, Takvorian AG, Rafalski M, Kasireddy-Polam P, Vig S, Dasgupta B, Zhang G, Molski TF, Wong H, Zaczek RC, Lodge NJ, Combs AP, Gilligan PJ, Trainor GL, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4986-9. doi: 10.1016/j.bmcl.2012.06.034. Epub 2012 Jun 16.

PMID:
22749422
27.

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE).

Boy KM, Guernon JM, Shi J, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Marcinkeviciene J, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Lentz KA, Bronson JJ, Olson RE, Macor JE, Thompson LA 3rd.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6916-24. doi: 10.1016/j.bmcl.2011.06.109. Epub 2011 Jun 30.

PMID:
21782431
28.

Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines.

Zuev D, Mattson RJ, Huang H, Mattson GK, Zueva L, Nielsen JM, Kozlowski ES, Huang XS, Wu D, Gao Q, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2484-8. doi: 10.1016/j.bmcl.2011.02.050. Epub 2011 Feb 17.

PMID:
21411322
29.

Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.

Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079.

PMID:
21078556
30.

Chiral separation of potent corticotropin-releasing factor-1 receptor antagonists by supercritical fluid chromatography.

Qian-Cutrone J, Hartz R, Ahuja VT, Vrudhula VM, Wu DR, Dalterio RA, Wang-Iverson D, Bronson JJ.

J Pharm Biomed Anal. 2011 Feb 20;54(3):602-6. doi: 10.1016/j.jpba.2010.09.031. Epub 2010 Oct 30.

PMID:
21036503
31.

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE.

ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10.

32.

5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.

Schmitz WD, Brenner AB, Bronson JJ, Ditta JL, Griffin CR, Li YW, Lodge NJ, Molski TF, Olson RE, Zhuo X, Macor JE.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3579-83. doi: 10.1016/j.bmcl.2010.04.121. Epub 2010 May 17.

PMID:
20483614
33.

Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Schmitz WD, Molski TF, Mattson GK, Lodge NJ, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1890-4. doi: 10.1016/j.bmcl.2010.01.129. Epub 2010 Feb 1.

PMID:
20176478
34.

A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.

Hartz RA, Ahuja VT, Zhuo X, Mattson RJ, Denhart DJ, Deskus JA, Vrudhula VM, Pan S, Ditta JL, Shu YZ, Grace JE, Lentz KA, Lelas S, Li YW, Molski TF, Krishnananthan S, Wong H, Qian-Cutrone J, Schartman R, Denton R, Lodge NJ, Zaczek R, Macor JE, Bronson JJ.

J Med Chem. 2009 Dec 10;52(23):7653-68. doi: 10.1021/jm900716v.

PMID:
19954247
35.

Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation.

Zhuo X, Hartz RA, Bronson JJ, Wong H, Ahuja VT, Vrudhula VM, Leet JE, Huang S, Macor JE, Shu YZ.

Drug Metab Dispos. 2010 Jan;38(1):5-15. doi: 10.1124/dmd.109.028910.

PMID:
19833844
36.

Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Arvanitis AG, Rafalski M, Yue EW, Denhart DJ, Schmitz WD, Ditta JL, Deskus JA, Brenner AB, Hobbs FW, Payne J, Lelas S, Li YW, Molski TF, Mattson GK, Peng Y, Wong H, Grace JE, Lentz KA, Qian-Cutrone J, Zhuo X, Shu YZ, Lodge NJ, Zaczek R, Combs AP, Olson RE, Bronson JJ, Mattson RJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4173-91. doi: 10.1021/jm900301y.

PMID:
19552437
37.

In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.

Hartz RA, Ahuja VT, Rafalski M, Schmitz WD, Brenner AB, Denhart DJ, Ditta JL, Deskus JA, Yue EW, Arvanitis AG, Lelas S, Li YW, Molski TF, Wong H, Grace JE, Lentz KA, Li J, Lodge NJ, Zaczek R, Combs AP, Olson RE, Mattson RJ, Bronson JJ, Macor JE.

J Med Chem. 2009 Jul 23;52(14):4161-72. doi: 10.1021/jm900302q. Erratum in: J Med Chem. 2009 Sep 24;52(18):5770.

PMID:
19552436
38.

The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.

Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH.

J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23.

39.

Amino-caprolactam derivatives as gamma-secretase inhibitors.

Parker MF, Bronson JJ, Barten DM, Corsa JA, Du W, Felsenstein KM, Guss VL, Izzarelli D, Loo A, McElhone KE, Marcin LR, Padmanabha R, Pak R, Polson CT, Toyn JH, Varma S, Wang J, Wong V, Zheng M, Roberts SB.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. Epub 2007 Aug 26.

PMID:
17869509
40.

N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.

Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Deshpande MS, Felsenstein KM, Guss VL, Hansel SB, Johnson G, Keavy DJ, Lau WY, Mock J, Prasad CV, Polson CT, Sloan CP, Smith DW, Wallace OB, Wang HH, Williams A, Zheng M.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. Epub 2007 Jun 10.

PMID:
17606371
41.

Cyclopentanone ring-cleaved pleuromutilin derivatives.

Springer DM, Bunker A, Luh BY, Sorenson ME, Goodrich JT, Bronson JJ, DenBleyker K, Dougherty TJ, Fung-Tomc J.

Eur J Med Chem. 2007 Jan;42(1):109-13. Epub 2006 Dec 6.

PMID:
17156897
42.

Synthesis and antibacterial activity of nocathiacin I analogues.

Naidu BN, Sorenson ME, Matiskella JD, Li W, Sausker JB, Zhang Y, Connolly TP, Lam KS, Bronson JJ, Pucci MJ, Yang H, Ueda Y.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3545-9. Epub 2006 Apr 18.

PMID:
16621551
43.

Progress in the discovery of BACE inhibitors.

Thompson LA, Bronson JJ, Zusi FC.

Curr Pharm Des. 2005;11(26):3383-404. Review.

PMID:
16250843
44.

Biaryl isoxazolinone antibacterial agents.

Quesnelle CA, Gill P, Roy S, Dodier M, Marinier A, Martel A, Snyder LB, D'Andrea SV, Bronson JJ, Frosco M, Beaulieu D, Warr GA, Denbleyker KL, Stickle TM, Yang H, Chaniewski SE, Ferraro CA, Taylor D, Russell JW, Santone KS, Clarke J, Drain RL, Knipe JO, Mosure K, Barrett JF.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2728-33.

PMID:
15869878
45.

Chemical conversion of nocathiacin I to nocathiacin II and a lactone analogue of glycothiohexide alpha.

Connolly TP, Regueiro-Ren A, Leet JE, Springer DM, Goodrich J, Huang XS, Pucci MJ, Clark JM, Bronson JJ, Ueda Y.

J Nat Prod. 2005 Apr;68(4):550-3.

PMID:
15844946
46.

Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts.

Naidu BN, Sorenson ME, Bronson JJ, Pucci MJ, Clark JM, Ueda Y.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2069-72.

PMID:
15808470
47.

Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.

Naidu BN, Sorenson ME, Zhang Y, Kim OK, Matiskella JD, Wichtowski JA, Connolly TP, Li W, Lam KS, Bronson JJ, Pucci MJ, Clark JM, Ueda Y.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5573-7.

PMID:
15482927
48.

Antimicrobial evaluation of nocathiacins, a thiazole peptide class of antibiotics.

Pucci MJ, Bronson JJ, Barrett JF, DenBleyker KL, Discotto LF, Fung-Tomc JC, Ueda Y.

Antimicrob Agents Chemother. 2004 Oct;48(10):3697-701.

49.

Discovery of isoxazolinone antibacterial agents. Nitrogen as a replacement for the stereogenic center found in oxazolidinone antibacterials.

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