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Page 1
Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Voight EA, Gomtsyan AR, Daanen JF, Perner RJ, Schmidt RG, Bayburt EK, DiDomenico S, McDonald HA, Puttfarcken PS, Chen J, Neelands TR, Bianchi BR, Han P, Reilly RM, Franklin PH, Segreti JA, Nelson RA, Su Z, King AJ, Polakowski JS, Baker SJ, Gauvin DM, Lewis LR, Mikusa JP, Joshi SK, Faltynek CR, Kym PR, Kort ME. Voight EA, et al. Among authors: bayburt ek. J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21. J Med Chem. 2014. PMID: 25100568
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, Didomenico S, Koenig JR, Turner S, Jinkerson T, Drizin I, Hannick SM, Macri BS, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter J, Stewart KD, Oie T, Jarvis MF, Surowy CS, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: bayburt ek. J Med Chem. 2005 Feb 10;48(3):744-52. doi: 10.1021/jm0492958. J Med Chem. 2005. PMID: 15689158
Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
Drizin I, Gomtsyan A, Bayburt EK, Schmidt RG, Zheng GZ, Perner RJ, DiDomenico S, Koenig JR, Turner SC, Jinkerson TK, Brown BS, Keddy RG, McDonald HA, Honore P, Wismer CT, Marsh KC, Wetter JM, Polakowski JS, Segreti JA, Jarvis MF, Faltynek CR, Lee CH. Drizin I, et al. Among authors: bayburt ek. Bioorg Med Chem. 2006 Jul 15;14(14):4740-9. doi: 10.1016/j.bmc.2006.03.027. Epub 2006 Apr 18. Bioorg Med Chem. 2006. PMID: 16621571
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
Gomtsyan A, Bayburt EK, Keddy R, Turner SC, Jinkerson TK, Didomenico S, Perner RJ, Koenig JR, Drizin I, McDonald HA, Surowy CS, Honore P, Mikusa J, Marsh KC, Wetter JM, Faltynek CR, Lee CH. Gomtsyan A, et al. Among authors: bayburt ek. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. doi: 10.1016/j.bmcl.2007.04.105. Epub 2007 May 3. Bioorg Med Chem Lett. 2007. PMID: 17507218
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Perner RJ, DiDomenico S, Koenig JR, Gomtsyan A, Bayburt EK, Schmidt RG, Drizin I, Zheng GZ, Turner SC, Jinkerson T, Brown BS, Keddy RG, Lukin K, McDonald HA, Honore P, Mikusa J, Marsh KC, Wetter JM, George KS, Jarvis MF, Faltynek CR, Lee CH. Perner RJ, et al. Among authors: bayburt ek. J Med Chem. 2007 Jul 26;50(15):3651-60. doi: 10.1021/jm070276i. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583335
Chroman and tetrahydroquinoline ureas as potent TRPV1 antagonists.
Schmidt RG, Bayburt EK, Latshaw SP, Koenig JR, Daanen JF, McDonald HA, Bianchi BR, Zhong C, Joshi S, Honore P, Marsh KC, Lee CH, Faltynek CR, Gomtsyan A. Schmidt RG, et al. Among authors: bayburt ek. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1338-41. doi: 10.1016/j.bmcl.2011.01.056. Epub 2011 Jan 21. Bioorg Med Chem Lett. 2011. PMID: 21315587
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR. Gomtsyan A, et al. Among authors: bayburt ek. J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2. J Med Chem. 2016. PMID: 27077528
Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia.
Honore P, Chandran P, Hernandez G, Gauvin DM, Mikusa JP, Zhong C, Joshi SK, Ghilardi JR, Sevcik MA, Fryer RM, Segreti JA, Banfor PN, Marsh K, Neelands T, Bayburt E, Daanen JF, Gomtsyan A, Lee CH, Kort ME, Reilly RM, Surowy CS, Kym PR, Mantyh PW, Sullivan JP, Jarvis MF, Faltynek CR. Honore P, et al. Pain. 2009 Mar;142(1-2):27-35. doi: 10.1016/j.pain.2008.11.004. Epub 2009 Jan 9. Pain. 2009. PMID: 19135797
22 results