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2-Nitrophenylcarbamoyl-(S)-prolyl-(S)-3-(2-naphthyl)alanyl-N-benzyl-N - methylamide (SDZ NKT 343), a potent human NK1 tachykinin receptor antagonist with good oral analgesic activity in chronic pain models.
Walpole C, Ko SY, Brown M, Beattie D, Campbell E, Dickenson F, Ewan S, Hughes GA, Lemaire M, Lerpiniere J, Patel S, Urban L. Walpole C, et al. Among authors: hughes ga. J Med Chem. 1998 Aug 13;41(17):3159-73. doi: 10.1021/jm970499g. J Med Chem. 1998. PMID: 9703462
Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Burgess GM, Perkins MN, Rang HP, Campbell EA, Brown MC, McIntyre P, Urban L, Dziadulewicz EK, Ritchie TJ, Hallett A, Snell CR, Wrigglesworth R, Lee W, Davis C, Phagoo SB, Davis AJ, Phillips E, Drake GS, Hughes GA, Dunstan A, Bloomfield GC. Burgess GM, et al. Among authors: hughes ga. Br J Pharmacol. 2000 Jan;129(1):77-86. doi: 10.1038/sj.bjp.0703012. Br J Pharmacol. 2000. PMID: 10694205 Free PMC article.
1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.
Dziadulewicz EK, Ritchie TJ, Hallett A, Snell CR, Ko SY, Wrigglesworth R, Hughes GA, Dunstan AR, Bloomfield GC, Drake GS, Brown MC, Lee W, Burgess GM, Davis C, Yaqoob M, Perkins MN, Campbell EA, Davis AJ, Rang HP. Dziadulewicz EK, et al. Among authors: hughes ga. J Med Chem. 2000 Mar 9;43(5):769-71. doi: 10.1021/jm991155o. J Med Chem. 2000. PMID: 10715143 No abstract available.
Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
Culshaw AJ, Bevan S, Christiansen M, Copp P, Davis A, Davis C, Dyson A, Dziadulewicz EK, Edwards L, Eggelte H, Fox A, Gentry C, Groarke A, Hallett A, Hart TW, Hughes GA, Knights S, Kotsonis P, Lee W, Lyothier I, McBryde A, McIntyre P, Paloumbis G, Panesar M, Patel S, Seiler MP, Yaqoob M, Zimmermann K. Culshaw AJ, et al. Among authors: hughes ga. J Med Chem. 2006 Jan 26;49(2):471-4. doi: 10.1021/jm051058x. J Med Chem. 2006. PMID: 16420034
Discovery of Icenticaftor (QBW251), a Cystic Fibrosis Transmembrane Conductance Regulator Potentiator with Clinical Efficacy in Cystic Fibrosis and Chronic Obstructive Pulmonary Disease.
Grand DL, Gosling M, Baettig U, Bahra P, Bala K, Brocklehurst C, Budd E, Butler R, Cheung AK, Choudhury H, Collingwood SP, Cox B, Danahay H, Edwards L, Everatt B, Glaenzel U, Glotin AL, Groot-Kormelink P, Hall E, Hatto J, Howsham C, Hughes G, King A, Koehler J, Kulkarni S, Lightfoot M, Nicholls I, Page C, Pergl-Wilson G, Popa MO, Robinson R, Rowlands D, Sharp T, Spendiff M, Stanley E, Steward O, Taylor RJ, Tranter P, Wagner T, Watson H, Williams G, Wright P, Young A, Sandham DA. Grand DL, et al. J Med Chem. 2021 Jun 10;64(11):7241-7260. doi: 10.1021/acs.jmedchem.1c00343. Epub 2021 May 24. J Med Chem. 2021. PMID: 34028270
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