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Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition.
Fish PV, Deur C, Gan X, Greene K, Hoople D, Mackenny M, Para KS, Reeves K, Ryckmans T, Stiff C, Stobie A, Wakenhut F, Whitlock GA. Fish PV, et al. Among authors: Whitlock GA. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2562-6. doi: 10.1016/j.bmcl.2008.03.050. Epub 2008 Mar 20. Bioorg Med Chem Lett. 2008. PMID: 18387300
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Jones P, Storer RI, Sabnis YA, Wakenhut FM, Whitlock GA, England KS, Mukaiyama T, Dehnhardt CM, Coe JW, Kortum SW, Chrencik JE, Brown DG, Jones RM, Murphy JR, Yeoh T, Morgan P, Kilty I. Jones P, et al. Among authors: Whitlock GA. J Med Chem. 2017 Jan 26;60(2):767-786. doi: 10.1021/acs.jmedchem.6b01634. Epub 2017 Jan 4. J Med Chem. 2017. PMID: 27983835
Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity.
Mowbray CE, Braillard S, Speed W, Glossop PA, Whitlock GA, Gibson KR, Mills JE, Brown AD, Gardner JM, Cao Y, Hua W, Morgans GL, Feijens PB, Matheeussen A, Maes LJ. Mowbray CE, et al. Among authors: Whitlock GA. J Med Chem. 2015 Dec 24;58(24):9615-24. doi: 10.1021/acs.jmedchem.5b01456. Epub 2015 Dec 4. J Med Chem. 2015. PMID: 26571076
Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors.
Storer RI, Brennan PE, Brown AD, Bungay PJ, Conlon KM, Corbett MS, DePianta RP, Fish PV, Heifetz A, Ho DK, Jessiman AS, McMurray G, de Oliveira CA, Roberts LR, Root JA, Shanmugasundaram V, Shapiro MJ, Skerten M, Westbrook D, Wheeler S, Whitlock GA, Wright J. Storer RI, et al. Among authors: Whitlock GA. J Med Chem. 2014 Jun 26;57(12):5258-69. doi: 10.1021/jm5003292. Epub 2014 Jun 17. J Med Chem. 2014. PMID: 24878222
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence.
Andrews MD, Fish PV, Blagg J, Brabham TK, Brennan PE, Bridgeland A, Brown AD, Bungay PJ, Conlon KM, Edmunds NJ, af Forselles K, Gibbons CP, Green MP, Hanton G, Holbrook M, Jessiman AS, McIntosh K, McMurray G, Nichols CL, Root JA, Storer RI, Sutton MR, Ward RV, Westbrook D, Whitlock GA. Andrews MD, et al. Among authors: Whitlock GA. Bioorg Med Chem Lett. 2011 May 1;21(9):2715-20. doi: 10.1016/j.bmcl.2010.11.120. Epub 2010 Dec 4. Bioorg Med Chem Lett. 2011. PMID: 21195614
Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Fray MJ, Fish PV, Allan GA, Bish G, Clarke N, Eccles R, Harrison AC, Le Net JL, Phillips SC, Regan N, Sobry C, Stobie A, Wakenhut F, Westbrook D, Westbrook SL, Whitlock GA. Fray MJ, et al. Among authors: Whitlock GA. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. doi: 10.1016/j.bmcl.2010.04.052. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471260
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Wakenhut F, Allan GA, Fish PV, Fray MJ, Harrison AC, McCoy R, Phillips SC, Ryckmans T, Stobie A, Westbrook D, Westbrook SL, Whitlock GA. Wakenhut F, et al. Among authors: Whitlock GA. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5078-81. doi: 10.1016/j.bmcl.2009.07.049. Epub 2009 Jul 31. Bioorg Med Chem Lett. 2009. PMID: 19647430
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