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Page 1
Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Steeneck C, Gege C, Kinzel O, Albers M, Kleymann G, Schlüter T, Schulz A, Xue X, Cummings MD, Fourie AM, Leonard KA, Scott B, Edwards JP, Hoffmann T, Goldberg SD. Steeneck C, et al. Among authors: scott b. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127174. doi: 10.1016/j.bmcl.2020.127174. Epub 2020 Apr 7. Bioorg Med Chem Lett. 2020. PMID: 32334912
3-Substituted Quinolines as RORγt Inverse Agonists.
Tanis VM, Venkatesan H, Cummings MD, Albers M, Kent Barbay J, Herman K, Kummer DA, Milligan C, Nelen MI, Nishimura R, Schlueter T, Scott B, Spurlino J, Wolin R, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Tanis VM, et al. Among authors: scott b. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1463-1470. doi: 10.1016/j.bmcl.2019.04.021. Epub 2019 Apr 12. Bioorg Med Chem Lett. 2019. PMID: 31010722
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Hoffmann T, Xue X, Cummings MD, Spurlino J, Milligan C, Fourie AM, Edwards JP, Leonard K, Coe K, Scott B, Pippel D, Goldberg SD. Gege C, et al. Among authors: scott b. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127205. doi: 10.1016/j.bmcl.2020.127205. Epub 2020 Apr 21. Bioorg Med Chem Lett. 2020. PMID: 32336498
1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.
Lebsack AD, Rech JC, Branstetter BJ, Hawryluk NA, Merit JE, Allison B, Rynberg R, Buma J, Rizzolio M, Swanson N, Ao H, Maher MP, Herrmann M, Freedman J, Scott BP, Luo L, Bhattacharya A, Wang Q, Chaplan SR, Wickenden AD, Breitenbucher JG. Lebsack AD, et al. Among authors: scott bp. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7142-6. doi: 10.1016/j.bmcl.2010.09.006. Epub 2010 Sep 7. Bioorg Med Chem Lett. 2010. PMID: 20932750
The SAR of brain penetration for a series of heteroaryl urea FAAH inhibitors.
Keith JM, Tichenor MS, Apodaca RL, Xiao W, Jones WM, Seierstad M, Pierce JM, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Wennerholm ML, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3109-3114. doi: 10.1016/j.bmcl.2016.05.001. Epub 2016 May 5. Bioorg Med Chem Lett. 2016. PMID: 27189675
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.
Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Guy Breitenbucher J. Lebsack AD, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):40-6. doi: 10.1016/j.bmcl.2008.11.024. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19038548
Novel ketooxazole based inhibitors of fatty acid amide hydrolase (FAAH).
Timmons A, Seierstad M, Apodaca R, Epperson M, Pippel D, Brown S, Chang L, Scott B, Webb M, Chaplan SR, Breitenbucher JG. Timmons A, et al. Among authors: scott b. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2109-13. doi: 10.1016/j.bmcl.2008.01.091. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18289847
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
Keith JM, Jones WM, Pierce JM, Seierstad M, Palmer JA, Webb M, Karbarz MJ, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Brown SM, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Keith JM, et al. Bioorg Med Chem Lett. 2014 Feb 1;24(3):737-41. doi: 10.1016/j.bmcl.2013.12.113. Epub 2014 Jan 6. Bioorg Med Chem Lett. 2014. PMID: 24433863
2,284 results