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72 results

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Page 1
The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Childers WE Jr, Havran LM, Asselin M, Bicksler JJ, Chong DC, Grosu GT, Shen Z, Abou-Gharbia MA, Bach AC 3rd, Harrison BL, Kagan N, Kleintop T, Magolda R, Marathias V, Robichaud AJ, Sabb AL, Zhang MY, Andree TH, Aschmies SH, Beyer C, Comery TA, Day M, Grauer SM, Hughes ZA, Rosenzweig-Lipson S, Platt B, Pulicicchio C, Smith DE, Sukoff-Rizzo SJ, Sullivan KM, Adedoyin A, Huselton C, Hirst WD. Childers WE Jr, et al. Among authors: magolda r. J Med Chem. 2010 May 27;53(10):4066-84. doi: 10.1021/jm1000908. J Med Chem. 2010. PMID: 20443629
Prodrugs of perzinfotel with improved oral bioavailability.
Baudy RB, Butera JA, Abou-Gharbia MA, Chen H, Harrison B, Jain U, Magolda R, Sze JY, Brandt MR, Cummons TA, Kowal D, Pangalos MN, Zupan B, Hoffmann M, May M, Mugford C, Kennedy J, Childers WE Jr. Baudy RB, et al. Among authors: magolda r. J Med Chem. 2009 Feb 12;52(3):771-8. doi: 10.1021/jm8011799. J Med Chem. 2009. PMID: 19146418
Preclinical characterization of WAY-211612: a dual 5-HT uptake inhibitor and 5-HT (1A) receptor antagonist and potential novel antidepressant.
Beyer CE, Lin Q, Platt B, Malberg J, Hornby G, Sullivan KM, Smith DL, Lock T, Mitchell PJ, Hatzenbuhler NT, Evrard DA, Harrison BL, Magolda R, Pangalos MN, Schechter LE, Rosenzweig-Lipson S, Andree TH. Beyer CE, et al. Among authors: magolda r. Br J Pharmacol. 2009 May;157(2):307-19. doi: 10.1111/j.1476-5381.2009.00146.x. Epub 2009 Mar 26. Br J Pharmacol. 2009. PMID: 19338583 Free PMC article.
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: magolda r. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.
Blass BE, Fensome A, Trybulski E, Magolda R, Gardell SJ, Liu K, Samuel M, Feingold I, Huselton C, Jackson CM, Djandjighian L, Ho D, Hennan J, Janusz JM. Blass BE, et al. Among authors: magolda r. J Med Chem. 2009 Nov 12;52(21):6531-4. doi: 10.1021/jm901042m. J Med Chem. 2009. PMID: 19888755
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Zhou P, Li Y, Fan Y, Wang Z, Chopra R, Olland A, Hu Y, Magolda RL, Pangalos M, Reinhart PH, Turner MJ, Bard J, Malamas MS, Robichaud AJ. Zhou P, et al. Among authors: magolda rl. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2326-9. doi: 10.1016/j.bmcl.2010.01.136. Epub 2010 Feb 12. Bioorg Med Chem Lett. 2010. PMID: 20202842
Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).
Pelletier JC, Chengalvala MV, Cottom JE, Feingold IB, Green DM, Hauze DB, Huselton CA, Jetter JW, Kopf GS, Lundquist JT, Magolda RL, Mann CW, Mehlmann JF, Rogers JF, Shanno LK, Adams WR, Tio CO, Wrobel JE. Pelletier JC, et al. Among authors: magolda rl. J Med Chem. 2009 Apr 9;52(7):2148-52. doi: 10.1021/jm801572m. J Med Chem. 2009. PMID: 19271735
Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS. Martone RL, et al. Among authors: magolda r. J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11. J Pharmacol Exp Ther. 2009. PMID: 19671883
72 results