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Page 1
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: drizin i. 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. 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: drizin i. 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: drizin i. J Med Chem. 2007 Jul 26;50(15):3651-60. doi: 10.1021/jm070276i. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583335
Discovery and biological evaluation of 5-aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Kort ME, Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Johnson MS, Pacofsky GJ, Thomas JB, Carroll WA, Krambis MJ, Liu D, Shieh CC, Zhang X, Hernandez G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Marsh KC, Murray BP, Liu J, Werness S, Faltynek CR, Krafte DS, Jarvis MF, Chapman ML, Marron BE. Kort ME, et al. Among authors: drizin i. J Med Chem. 2008 Feb 14;51(3):407-16. doi: 10.1021/jm070637u. Epub 2008 Jan 5. J Med Chem. 2008. PMID: 18176998
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain.
Drizin I, Gregg RJ, Scanio MJ, Shi L, Gross MF, Atkinson RN, Thomas JB, Johnson MS, Carroll WA, Marron BE, Chapman ML, Liu D, Krambis MJ, Shieh CC, Zhang X, Hernandez G, Gauvin DM, Mikusa JP, Zhu CZ, Joshi S, Honore P, Marsh KC, Roeloffs R, Werness S, Krafte DS, Jarvis MF, Faltynek CR, Kort ME. Drizin I, et al. Bioorg Med Chem. 2008 Jun 15;16(12):6379-86. doi: 10.1016/j.bmc.2008.05.003. Epub 2008 May 6. Bioorg Med Chem. 2008. PMID: 18501613
Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
Cowart MD, Altenbach RJ, Liu H, Hsieh GC, Drizin I, Milicic I, Miller TR, Witte DG, Wishart N, Fix-Stenzel SR, McPherson MJ, Adair RM, Wetter JM, Bettencourt BM, Marsh KC, Sullivan JP, Honore P, Esbenshade TA, Brioni JD. Cowart MD, et al. Among authors: drizin i. J Med Chem. 2008 Oct 23;51(20):6547-57. doi: 10.1021/jm800670r. Epub 2008 Sep 26. J Med Chem. 2008. PMID: 18817367
Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE. Kort ME, et al. Among authors: drizin i. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6812-5. doi: 10.1016/j.bmcl.2010.08.121. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855211
Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain.
Scanio MJ, Shi L, Drizin I, Gregg RJ, Atkinson RN, Thomas JB, Johnson MS, Chapman ML, Liu D, Krambis MJ, Liu Y, Shieh CC, Zhang X, Simler GH, Joshi S, Honore P, Marsh KC, Knox A, Werness S, Antonio B, Krafte DS, Jarvis MF, Faltynek CR, Marron BE, Kort ME. Scanio MJ, et al. Among authors: drizin i. Bioorg Med Chem. 2010 Nov 15;18(22):7816-25. doi: 10.1016/j.bmc.2010.09.057. Epub 2010 Sep 29. Bioorg Med Chem. 2010. PMID: 20965738
19 results