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Page 1
Discovery of orally bioavailable cathepsin S inhibitors for the reversal of neuropathic pain.
Irie O, Kosaka T, Ehara T, Yokokawa F, Kanazawa T, Hirao H, Iwasaki A, Sakaki J, Teno N, Hitomi Y, Iwasaki G, Fukaya H, Nonomura K, Tanabe K, Koizumi S, Uchiyama N, Bevan SJ, Malcangio M, Gentry C, Fox AJ, Yaqoob M, Culshaw AJ, Allan Hallett. Irie O, et al. Among authors: yaqoob m. J Med Chem. 2008 Sep 25;51(18):5502-5. doi: 10.1021/jm800839j. J Med Chem. 2008. PMID: 18754655
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Dziadulewicz EK, Bevan SJ, Brain CT, Coote PR, Culshaw AJ, Davis AJ, Edwards LJ, Fisher AJ, Fox AJ, Gentry C, Groarke A, Hart TW, Huber W, James IF, Kesingland A, La Vecchia L, Loong Y, Lyothier I, McNair K, O'Farrell C, Peacock M, Portmann R, Schopfer U, Yaqoob M, Zadrobilek J. Dziadulewicz EK, et al. Among authors: yaqoob m. J Med Chem. 2007 Aug 9;50(16):3851-6. doi: 10.1021/jm070317a. Epub 2007 Jul 14. J Med Chem. 2007. PMID: 17630726
Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-cyanopyrimidines. Part 2.
Irie O, Kosaka T, Kishida M, Sakaki J, Masuya K, Konishi K, Yokokawa F, Ehara T, Iwasaki A, Iwaki Y, Hitomi Y, Toyao A, Gunji H, Teno N, Iwasaki G, Hirao H, Kanazawa T, Tanabe K, Hiestand PC, Malcangio M, Fox AJ, Bevan SJ, Yaqoob M, Culshaw AJ, Hart TW, Hallett A. Irie O, et al. Among authors: yaqoob m. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5280-4. doi: 10.1016/j.bmcl.2008.08.067. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18783943
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: yaqoob m. J Med Chem. 2006 Jan 26;49(2):471-4. doi: 10.1021/jm051058x. J Med Chem. 2006. PMID: 16420034
Nonpeptide bradykinin B2 receptor antagonists: conversion of rodent-selective bradyzide analogues into potent, orally-active human bradykinin B2 receptor antagonists.
Dziadulewicz EK, Ritchie TJ, Hallett A, Snell CR, Davies JW, Wrigglesworth R, Dunstan AR, Bloomfield GC, Drake GS, McIntyre P, Brown MC, Burgess GM, Lee W, Davis C, Yaqoob M, Phagoo SB, Phillips E, Perkins MN, Campbell EA, Davis AJ, Rang HP. Dziadulewicz EK, et al. Among authors: yaqoob m. J Med Chem. 2002 May 23;45(11):2160-72. doi: 10.1021/jm0111088. J Med Chem. 2002. PMID: 12014954
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: yaqoob m. J Med Chem. 2000 Mar 9;43(5):769-71. doi: 10.1021/jm991155o. J Med Chem. 2000. PMID: 10715143 No abstract available.
480 results