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Page 1
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, Cottney JE, Deehan M, Easson AM, Ecker D, Edwards D, Epemolu O, Evans L, Fields R, Francis S, Harradine P, Jeremiah F, Kiyoi T, McArthur D, Morrison A, Passier P, Pick J, Schnabel PG, Schulz J, Steinbrede H, Walker G, Westwood P, Wishart G, Udo de Haes J. Ratcliffe P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2541-6. doi: 10.1016/j.bmcl.2011.02.023. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21411321
The first potent and selective inhibitors of the glycine transporter type 2.
Caulfield WL, Collie IT, Dickins RS, Epemolu O, McGuire R, Hill DR, McVey G, Morphy JR, Rankovic Z, Sundaram H. Caulfield WL, et al. Among authors: epemolu o. J Med Chem. 2001 Aug 16;44(17):2679-82. doi: 10.1021/jm0011272. J Med Chem. 2001. PMID: 11495577 No abstract available.
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G. Reid M, et al. Among authors: o donnell ec, epemolu o. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20471831
Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ. Ray P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Jan 1;21(1):97-101. doi: 10.1016/j.bmcl.2010.11.060. Epub 2010 Nov 19. Bioorg Med Chem Lett. 2011. PMID: 21145740
Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Ray P, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21251828
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L. Kiyoi T, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316962
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298).
Soares P, Gadd MS, Frost J, Galdeano C, Ellis L, Epemolu O, Rocha S, Read KD, Ciulli A. Soares P, et al. Among authors: epemolu o. J Med Chem. 2018 Jan 25;61(2):599-618. doi: 10.1021/acs.jmedchem.7b00675. Epub 2017 Sep 18. J Med Chem. 2018. PMID: 28853884 Free PMC article.
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH. Brand S, et al. Among authors: epemolu o. J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27. J Med Chem. 2017. PMID: 28844141 Free PMC article.
Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1.
Bell M, Foley D, Naylor C, Robinson C, Riley J, Epemolu O, Scullion P, Shishikura Y, Katz E, McLean WHI, Wyatt P, Read KD, Woodland A. Bell M, et al. Among authors: epemolu o. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3255-3259. doi: 10.1016/j.bmcl.2018.07.044. Epub 2018 Jul 30. Bioorg Med Chem Lett. 2018. PMID: 30143424 Free PMC article.
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity.
Thomas MG, De Rycker M, Wall RJ, Spinks D, Epemolu O, Manthri S, Norval S, Osuna-Cabello M, Patterson S, Riley J, Simeons FRC, Stojanovski L, Thomas J, Thompson S, Naylor C, Fiandor JM, Wyatt PG, Marco M, Wyllie S, Read KD, Miles TJ, Gilbert IH. Thomas MG, et al. Among authors: epemolu o. J Med Chem. 2020 Sep 10;63(17):9523-9539. doi: 10.1021/acs.jmedchem.0c00705. Epub 2020 Aug 13. J Med Chem. 2020. PMID: 32663005 Free PMC article.
39 results