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Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.
Di Fabio R, Pellacani A, Faedo S, Roth A, Piccoli L, Gerrard P, Porter RA, Johnson CN, Thewlis K, Donati D, Stasi L, Spada S, Stemp G, Nash D, Branch C, Kindon L, Massagrande M, Poffe A, Braggio S, Chiarparin E, Marchioro C, Ratti E, Corsi M. Di Fabio R, et al. Among authors: porter ra. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. doi: 10.1016/j.bmcl.2011.06.086. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21831639
New quinoline NK3 receptor antagonists with CNS activity.
Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA. Smith PW, et al. Bioorg Med Chem Lett. 2009 Feb 1;19(3):837-40. doi: 10.1016/j.bmcl.2008.12.005. Epub 2008 Dec 7. Bioorg Med Chem Lett. 2009. PMID: 19117759
Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization.
Zirimwabagabo JO, Jailani ABA, Avgoustou P, Tozer MJ, Gibson KR, Glossop PA, Mills JEJ, Porter RA, Blaney P, Wang N, Skerry TM, Richards GO, Harrity JPA. Zirimwabagabo JO, et al. Among authors: porter ra. J Med Chem. 2021 Mar 25;64(6):3299-3319. doi: 10.1021/acs.jmedchem.0c02191. Epub 2021 Mar 5. J Med Chem. 2021. PMID: 33666424 Free PMC article.
Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors.
Harrison D, Boutard N, Brzozka K, Bugaj M, Chmielewski S, Cierpich A, Doedens JR, Fabritius CRY, Gabel CA, Galezowski M, Kowalczyk P, Levenets O, Mroczkowska M, Palica K, Porter RA, Schultz D, Sowinska M, Topolnicki G, Urbanski P, Woyciechowski J, Watt AP. Harrison D, et al. Among authors: porter ra. Bioorg Med Chem Lett. 2020 Dec 1;30(23):127560. doi: 10.1016/j.bmcl.2020.127560. Epub 2020 Sep 18. Bioorg Med Chem Lett. 2020. PMID: 32956781
Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor.
Avgoustou P, Jailani ABA, Zirimwabagabo JO, Tozer MJ, Gibson KR, Glossop PA, Mills JEJ, Porter RA, Blaney P, Bungay PJ, Wang N, Shaw AP, Bigos KJA, Holmes JL, Warrington JI, Skerry TM, Harrity JPA, Richards GO. Avgoustou P, et al. Among authors: porter ra. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):706-719. doi: 10.1021/acsptsci.0c00032. eCollection 2020 Aug 14. ACS Pharmacol Transl Sci. 2020. PMID: 32832872 Free PMC article.
65 results