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Items: 1 to 50 of 55

1.

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.

2.

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K.

J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16.

PMID:
30256636
3.

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.

Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS.

Antimicrob Agents Chemother. 2018 Nov 26;62(12). pii: e00261-18. doi: 10.1128/AAC.00261-18. Print 2018 Dec.

PMID:
30249687
4.

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):.

PMID:
29941635
5.

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.

Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K.

J Med Chem. 2018 Jul 12;61(13):5692-5703. doi: 10.1021/acs.jmedchem.8b00648. Epub 2018 Jun 27.

PMID:
29889526
6.

Synthesis and biological evaluation of aryl-oxadiazoles as inhibitors of Mycobacterium tuberculosis.

Martinez-Grau MA, Valcarcel ICG, Early JV, Gessner RK, de Melo CS, de la Nava EMM, Korkegian A, Ovechkina Y, Flint L, Gravelle A, Cramer JW, Desai PV, Street LJ, Odingo J, Masquelin T, Chibale K, Parish T.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1758-1764. doi: 10.1016/j.bmcl.2018.04.028. Epub 2018 Apr 13.

7.

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K.

J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27.

PMID:
29665687
8.

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization.

Murugesan D, Ray PC, Bayliss T, Prosser GA, Harrison JR, Green K, Soares de Melo C, Feng TS, Street LJ, Chibale K, Warner DF, Mizrahi V, Epemolu O, Scullion P, Ellis L, Riley J, Shishikura Y, Ferguson L, Osuna-Cabello M, Read KD, Green SR, Lamprecht DA, Finin PM, Steyn AJC, Ioerger TR, Sacchettini J, Rhee KY, Arora K, Barry CE 3rd, Wyatt PG, Boshoff HIM.

ACS Infect Dis. 2018 Jun 8;4(6):954-969. doi: 10.1021/acsinfecdis.7b00275. Epub 2018 Mar 26.

9.

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials.

van der Watt ME, Reader J, Churchyard A, Nondaba SH, Lauterbach SB, Niemand J, Abayomi S, van Biljon RA, Connacher JI, van Wyk RDJ, Le Manach C, Paquet T, González Cabrera D, Brunschwig C, Theron A, Lozano-Arias S, Rodrigues JFI, Herreros E, Leroy D, Duffy J, Street LJ, Chibale K, Mancama D, Coetzer TL, Birkholtz LM.

J Antimicrob Chemother. 2018 May 1;73(5):1279-1290. doi: 10.1093/jac/dky008.

PMID:
29420756
10.

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.

Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K.

J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7.

11.

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.

12.

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle.

Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K.

J Med Chem. 2016 Nov 10;59(21):9890-9905. Epub 2016 Oct 26.

PMID:
27748596
13.

Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.

van der Westhuyzen R, Winks S, Wilson CR, Boyle GA, Gessner RK, Soares de Melo C, Taylor D, de Kock C, Njoroge M, Brunschwig C, Lawrence N, Rao SP, Sirgel F, van Helden P, Seldon R, Moosa A, Warner DF, Arista L, Manjunatha UH, Smith PW, Street LJ, Chibale K.

J Med Chem. 2015 Dec 10;58(23):9371-81. doi: 10.1021/acs.jmedchem.5b01542. Epub 2015 Nov 20.

PMID:
26551248
14.

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.

Soares de Melo C, Feng TS, van der Westhuyzen R, Gessner RK, Street LJ, Morgans GL, Warner DF, Moosa A, Naran K, Lawrence N, Boshoff HI, Barry CE 3rd, Harris CJ, Gordon R, Chibale K.

Bioorg Med Chem. 2015 Nov 15;23(22):7240-50. doi: 10.1016/j.bmc.2015.10.021. Epub 2015 Oct 22. Erratum in: Bioorg Med Chem. 2016 Jan 15;24(2):314. Candice, Soares de Melo [corrected to Soares de Melo, Candice].

PMID:
26522089
15.

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K.

J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2.

PMID:
26502160
16.

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

Gonzàlez Cabrera D, Douelle F, Le Manach C, Han Z, Paquet T, Taylor D, Njoroge M, Lawrence N, Wiesner L, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K.

J Med Chem. 2015 Sep 24;58(18):7572-9. doi: 10.1021/acs.jmedchem.5b01156. Epub 2015 Sep 8.

PMID:
26322748
17.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

Le Manach C, Paquet T, Gonzàlez Cabrera D, Younis Y, Taylor D, Wiesner L, Lawrence N, Schwager S, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K.

J Med Chem. 2014 Nov 13;57(21):8839-48. doi: 10.1021/jm500887k. Epub 2014 Oct 23.

PMID:
25313449
18.

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

Le Manach C, Gonzàlez Cabrera D, Douelle F, Nchinda AT, Younis Y, Taylor D, Wiesner L, White KL, Ryan E, March C, Duffy S, Avery VM, Waterson D, Witty MJ, Wittlin S, Charman SA, Street LJ, Chibale K.

J Med Chem. 2014 Mar 27;57(6):2789-98. doi: 10.1021/jm500098s. Epub 2014 Mar 13.

PMID:
24568587
19.

2,4-Diaminothienopyrimidines as orally active antimalarial agents.

González Cabrera D, Le Manach C, Douelle F, Younis Y, Feng TS, Paquet T, Nchinda AT, Street LJ, Taylor D, de Kock C, Wiesner L, Duffy S, White KL, Zabiulla KM, Sambandan Y, Bashyam S, Waterson D, Witty MJ, Charman SA, Avery VM, Wittlin S, Chibale K.

J Med Chem. 2014 Feb 13;57(3):1014-22. doi: 10.1021/jm401760c. Epub 2014 Jan 28.

PMID:
24446664
20.

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.

Younis Y, Douelle F, González Cabrera D, Le Manach C, Nchinda AT, Paquet T, Street LJ, White KL, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Wittlin S, Charman SA, Chibale K.

J Med Chem. 2013 Nov 14;56(21):8860-71. doi: 10.1021/jm401278d. Epub 2013 Oct 29.

PMID:
24099149
21.

Cell-based medicinal chemistry optimization of high throughput screening hits for orally active antimalarials. Part 2: hits from SoftFocus kinase and other libraries.

Younis Y, Street LJ, Waterson D, Witty MJ, Chibale K.

J Med Chem. 2013 Oct 24;56(20):7750-4. doi: 10.1021/jm400279y. Epub 2013 Aug 30. Review.

PMID:
23927599
22.

Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines.

González Cabrera D, Douelle F, Younis Y, Feng TS, Le Manach C, Nchinda AT, Street LJ, Scheurer C, Kamber J, White KL, Montagnat OD, Ryan E, Katneni K, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Charman SA, Wittlin S, Chibale K.

J Med Chem. 2012 Dec 27;55(24):11022-30. doi: 10.1021/jm301476b. Epub 2012 Dec 14.

PMID:
23189922
23.

Benzobistriazinones and related heterocyclic ring systems as potent, orally bioavailable positive allosteric AMPA receptor modulators.

Mueller R, Rachwal S, Varney MA, Johnson SA, Alisala K, Zhong S, Li YX, Haroldsen P, Herbst T, Street LJ.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7455-9. doi: 10.1016/j.bmcl.2011.09.132. Epub 2011 Oct 8.

PMID:
22056742
24.

Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.

Mueller R, Rachwal S, Lee S, Zhong S, Li YX, Haroldsen P, Herbst T, Tanimura S, Varney M, Johnson S, Rogers G, Street LJ.

Bioorg Med Chem Lett. 2011 Oct 15;21(20):6170-5. doi: 10.1016/j.bmcl.2011.07.098. Epub 2011 Aug 12.

PMID:
21889339
25.

Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.

Blackaby WP, Lewis RT, Thomson JL, Jennings AS, Goodacre SC, Street LJ, MacLeod AM, Pike A, Wood S, Thomas S, Brown TA, Smith A, Pillai G, Almond S, Guscott MR, Burns HD, Eng W, Ryan C, Cook J, Hamill TG.

ACS Med Chem Lett. 2010 Jun 25;1(7):350-4. doi: 10.1021/ml1001085. eCollection 2010 Oct 14.

26.

Preclinical and clinical pharmacology of TPA023B, a GABAA receptor α2/α3 subtype-selective partial agonist.

Atack JR, Hallett DJ, Tye S, Wafford KA, Ryan C, Sanabria-Bohórquez SM, Eng WS, Gibson RE, Burns HD, Dawson GR, Carling RW, Street LJ, Pike A, De Lepeleire I, Van Laere K, Bormans G, de Hoon JN, Van Hecken A, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):329-44. doi: 10.1177/0269881109354928. Epub 2010 Feb 15.

PMID:
20156926
27.

MRK-409 (MK-0343), a GABAA receptor subtype-selective partial agonist, is a non-sedating anxiolytic in preclinical species but causes sedation in humans.

Atack JR, Wafford KA, Street LJ, Dawson GR, Tye S, Van Laere K, Bormans G, Sanabria-Bohórquez SM, De Lepeleire I, de Hoon JN, Van Hecken A, Burns HD, McKernan RM, Murphy MG, Hargreaves RJ.

J Psychopharmacol. 2011 Mar;25(3):314-28. doi: 10.1177/0269881109354927. Epub 2010 Feb 10.

PMID:
20147571
28.

Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.

Thomson JL, Blackaby WP, Jennings AS, Goodacre SC, Pike A, Thomas S, Brown TA, Smith A, Pillai G, Street LJ, Lewis RT.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2235-9. doi: 10.1016/j.bmcl.2009.02.102. Epub 2009 Feb 28.

PMID:
19318248
29.

2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.

Carling RW, Russell MG, Moore KW, Mitchinson A, Guiblin A, Smith A, Wafford KA, Marshall G, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3550-4. Epub 2006 Apr 18.

PMID:
16621541
30.

Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.

Russell MG, Carling RW, Street LJ, Hallett DJ, Goodacre S, Mezzogori E, Reader M, Cook SM, Bromidge FA, Newman R, Smith AJ, Wafford KA, Marshall GR, Reynolds DS, Dias R, Ferris P, Stanley J, Lincoln R, Tye SJ, Sheppard WF, Sohal B, Pike A, Dominguez M, Atack JR, Castro JL.

J Med Chem. 2006 Feb 23;49(4):1235-8.

PMID:
16480260
31.

Imidazo[1,2-a]pyrimidines as functionally selective GABA(A) ligands.

Blackaby WP, Atack JR, Bromidge F, Castro JL, Goodacre SC, Hallett DJ, Lewis RT, Marshall GR, Pike A, Smith AJ, Street LJ, Tattersall DF, Wafford KA.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1175-9. Epub 2006 Jan 6.

PMID:
16406613
32.

Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.

Goodacre SC, Street LJ, Hallett DJ, Crawforth JM, Kelly S, Owens AP, Blackaby WP, Lewis RT, Stanley J, Smith AJ, Ferris P, Sohal B, Cook SM, Pike A, Brown N, Wafford KA, Marshall G, Castro JL, Atack JR.

J Med Chem. 2006 Jan 12;49(1):35-8.

PMID:
16392789
33.

Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Jennings AS, Lewis RT, Russell MG, Hallett DJ, Street LJ, Castro JL, Atack JR, Cook SM, Lincoln R, Stanley J, Smith AJ, Reynolds DS, Sohal B, Pike A, Marshall GR, Wafford KA, Sheppard WF, Tye SJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1477-80. Epub 2006 Jan 4.

PMID:
16386900
34.

Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.

Goodacre SC, Hallett DJ, Carling RW, Castro JL, Reynolds DS, Pike A, Wafford KA, Newman R, Atack JR, Street LJ.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1582-5. Epub 2005 Dec 27.

PMID:
16384707
35.

Evidence for a significant role of alpha 3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines.

Dias R, Sheppard WF, Fradley RL, Garrett EM, Stanley JL, Tye SJ, Goodacre S, Lincoln RJ, Cook SM, Conley R, Hallett D, Humphries AC, Thompson SA, Wafford KA, Street LJ, Castro JL, Whiting PJ, Rosahl TW, Atack JR, McKernan RM, Dawson GR, Reynolds DS.

J Neurosci. 2005 Nov 16;25(46):10682-8.

36.

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.

Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ.

J Med Chem. 2005 Nov 17;48(23):7089-92.

PMID:
16279764
37.

Pyrazolopyridinones as functionally selective GABAA ligands.

Blackaby WP, Atack JR, Bromidge F, Lewis R, Russell MG, Smith A, Wafford K, McKernan RM, Street LJ, Castro JL.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):4998-5002.

PMID:
16153832
38.

Synthesis and biological evaluation of 3-heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and analogues as subtype-selective inverse agonists for the GABA(A)alpha5 benzodiazepine binding site.

Street LJ, Sternfeld F, Jelley RA, Reeve AJ, Carling RW, Moore KW, McKernan RM, Sohal B, Cook S, Pike A, Dawson GR, Bromidge FA, Wafford KA, Seabrook GR, Thompson SA, Marshall G, Pillai GV, Castro JL, Atack JR, MacLeod AM.

J Med Chem. 2004 Jul 1;47(14):3642-57.

PMID:
15214791
39.

2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor.

Mitchinson A, Atack JR, Blurton P, Carling RW, Castro JL, Curley KS, Russell MG, Marshall G, McKernan RM, Moore KW, Narquizian R, Smith A, Street LJ, Thompson SA, Wafford K.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.

PMID:
15177449
40.

Selective, orally active gamma-aminobutyric acidA alpha5 receptor inverse agonists as cognition enhancers.

Sternfeld F, Carling RW, Jelley RA, Ladduwahetty T, Merchant KJ, Moore KW, Reeve AJ, Street LJ, O'Connor D, Sohal B, Atack JR, Cook S, Seabrook G, Wafford K, Tattersall FD, Collinson N, Dawson GR, Castro JL, MacLeod AM.

J Med Chem. 2004 Apr 22;47(9):2176-9.

PMID:
15084116
41.

3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor ligands with alpha 2, alpha 3, and alpha 5-subtype binding selectivity over alpha 1.

Carling RW, Moore KW, Street LJ, Wild D, Isted C, Leeson PD, Thomas S, O'Connor D, McKernan RM, Quirk K, Cook SM, Atack JR, Wafford KA, Thompson SA, Dawson GR, Ferris P, Castro JL.

J Med Chem. 2004 Mar 25;47(7):1807-22.

PMID:
15027873
42.

Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.

Crawforth J, Atack JR, Cook SM, Gibson KR, Nadin A, Owens AP, Pike A, Rowley M, Smith AJ, Sohal B, Sternfeld F, Wafford K, Street LJ.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1679-82.

PMID:
15026049
43.

Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour.

McCabe C, Shaw D, Atack JR, Street LJ, Wafford KA, Dawson GR, Reynolds DS, Leslie JC.

Neuropharmacology. 2004 Feb;46(2):171-8.

PMID:
14680756
44.

Sedative but not anxiolytic properties of benzodiazepines are mediated by the GABA(A) receptor alpha1 subtype.

McKernan RM, Rosahl TW, Reynolds DS, Sur C, Wafford KA, Atack JR, Farrar S, Myers J, Cook G, Ferris P, Garrett L, Bristow L, Marshall G, Macaulay A, Brown N, Howell O, Moore KW, Carling RW, Street LJ, Castro JL, Ragan CI, Dawson GR, Whiting PJ.

Nat Neurosci. 2000 Jun;3(6):587-92.

PMID:
10816315
45.

3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.

Chambers MS, Street LJ, Goodacre S, Hobbs SC, Hunt P, Jelley RA, Matassa VG, Reeve AJ, Sternfeld F, Beer MS, Stanton JA, Rathbone D, Watt AP, MacLeod AM.

J Med Chem. 1999 Feb 25;42(4):691-705.

PMID:
10052976
46.

Synthesis and serotonergic activity of 3-[2-(pyrrolidin-1-yl)ethyl]indoles: potent agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B receptor.

Sternfeld F, Guiblin AR, Jelley RA, Matassa VG, Reeve AJ, Hunt PA, Beer MS, Heald A, Stanton JA, Sohal B, Watt AP, Street LJ.

J Med Chem. 1999 Feb 25;42(4):677-90.

PMID:
10052975
47.

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.

MacLeod AM, Street LJ, Reeve AJ, Jelley RA, Sternfeld F, Beer MS, Stanton JA, Watt AP, Rathbone D, Matassa VG.

J Med Chem. 1997 Oct 24;40(22):3501-3. No abstract available.

PMID:
9357515
48.

3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.

Castro JL, Street LJ, Guiblin AR, Jelley RA, Russell MG, Sternfeld F, Beer MS, Stanton JA, Matassa VG.

J Med Chem. 1997 Oct 24;40(22):3497-500. No abstract available.

PMID:
9357514
49.

Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.

Street LJ, Baker R, Davey WB, Guiblin AR, Jelley RA, Reeve AJ, Routledge H, Sternfeld F, Watt AP, Beer MS, et al.

J Med Chem. 1995 May 12;38(10):1799-810.

PMID:
7752204
50.

L-694,247: a potent 5-HT1D receptor agonist.

Beer MS, Stanton JA, Bevan Y, Heald A, Reeve AJ, Street LJ, Matassa VG, Hargreaves RJ, Middlemiss DN.

Br J Pharmacol. 1993 Nov;110(3):1196-200.

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