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4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.
Procopiou PA, Ancliff RA, Bamford MJ, Browning C, Connor H, Davies S, Fogden YC, Hodgson ST, Holmes DS, Looker BE, Morriss KM, Parr CA, Pickup EA, Sehmi SS, White GV, Watts CJ, Wilson DM, Woodrow MD. Procopiou PA, et al. Among authors: holmes ds. J Med Chem. 2007 Dec 27;50(26):6706-17. doi: 10.1021/jm0708228. Epub 2007 Dec 6. J Med Chem. 2007. PMID: 18052318
GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.
Pearce AC, Bamford MJ, Barber R, Bridges A, Convery MA, Demetriou C, Evans S, Gobbetti T, Hirst DJ, Holmes DS, Hutchinson JP, Jayne S, Lezina L, McCabe MT, Messenger C, Morley J, Musso MC, Scott-Stevens P, Manso AS, Schofield J, Slocombe T, Somers D, Walker AL, Wyce A, Zhang XP, Wagner SD. Pearce AC, et al. Among authors: holmes ds. J Biol Chem. 2021 Aug;297(2):100928. doi: 10.1016/j.jbc.2021.100928. Epub 2021 Jul 15. J Biol Chem. 2021. PMID: 34274316 Free PMC article.
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.
Procopiou PA, Ford AJ, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Looker BE, Vile S, Clark KL, Saunders KA, Slack RJ, Watts CJ. Procopiou PA, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2017 Nov 1;27(21):4914-4919. doi: 10.1016/j.bmcl.2017.09.020. Epub 2017 Sep 9. Bioorg Med Chem Lett. 2017. PMID: 28958623
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight 'molecular budget'.
Hirst DJ, Brandt M, Bruton G, Christodoulou E, Cutler L, Deeks N, Goodacre JD, Jack T, Lindon M, Miah A, Page K, Parr N, Shukla L, Sims M, Thomas P, Thorpe J, Holmes DS. Hirst DJ, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2020 Nov 1;30(21):127533. doi: 10.1016/j.bmcl.2020.127533. Epub 2020 Sep 10. Bioorg Med Chem Lett. 2020. PMID: 32919012
Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: holmes ds. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
The discovery of potent and selective kynurenine 3-monooxygenase inhibitors for the treatment of acute pancreatitis.
Liddle J, Beaufils B, Binnie M, Bouillot A, Denis AA, Hann MM, Haslam CP, Holmes DS, Hutchinson JP, Kranz M, McBride A, Mirguet O, Mole DJ, Mowat CG, Pal S, Rowland P, Trottet L, Uings IJ, Walker AL, Webster SP. Liddle J, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2017 May 1;27(9):2023-2028. doi: 10.1016/j.bmcl.2017.02.078. Epub 2017 Mar 9. Bioorg Med Chem Lett. 2017. PMID: 28336141 Free article.
245 results