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Page 1
Identification of biaryl sulfone derivatives as antagonists of the histamine H₃ receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916).
Semple G, Santora VJ, Smith JM, Covel JA, Hayashi R, Gallardo C, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Smith BM, Ren A, Suarez M, Frazer J, Edwards JE, Hart R, Hauser EK, Lorea J, Grottick AJ. Semple G, et al. Among authors: covel ja. Bioorg Med Chem Lett. 2012 Jan 1;22(1):71-5. doi: 10.1016/j.bmcl.2011.11.075. Epub 2011 Nov 30. Bioorg Med Chem Lett. 2012. PMID: 22172695
A new family of H3 receptor antagonists based on the natural product Conessine.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Sengupta D, Duffield JJ, Semple G, Webb RR, Sage C, Ren A, Pereira G, Knudsen J, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Whelan K, Grottick AJ. Santora VJ, et al. Among authors: covel ja. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1490-4. doi: 10.1016/j.bmcl.2007.12.059. Epub 2007 Dec 25. Bioorg Med Chem Lett. 2008. PMID: 18194865
Novel H3 receptor antagonists with improved pharmacokinetic profiles.
Santora VJ, Covel JA, Hayashi R, Hofilena BJ, Ibarra JB, Pulley MD, Weinhouse MI, Semple G, Ren A, Pereira G, Edwards JE, Suarez M, Frazer J, Thomsen W, Hauser E, Lorea J, Grottick AJ. Santora VJ, et al. Among authors: covel ja. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4133-6. doi: 10.1016/j.bmcl.2008.05.086. Epub 2008 May 24. Bioorg Med Chem Lett. 2008. PMID: 18554904
Design and evaluation of novel biphenyl sulfonamide derivatives with potent histamine H(3) receptor inverse agonist activity.
Covel JA, Santora VJ, Smith JM, Hayashi R, Gallardo C, Weinhouse MI, Ibarra JB, Schultz JA, Park DM, Estrada SA, Hofilena BJ, Pulley MD, Smith BM, Ren A, Suarez M, Frazer J, Edwards J, Hauser EK, Lorea J, Semple G, Grottick AJ. Covel JA, et al. J Med Chem. 2009 Sep 24;52(18):5603-11. doi: 10.1021/jm900857n. J Med Chem. 2009. PMID: 19722526
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity.
Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Dosa PI, Covel JA, Ren A, Webb RR, Beeley NR, Martin M, Morgan M, Espitia S, Saldana HR, Bjenning C, Whelan KT, Grottick AJ, Menzaghi F, Thomsen WJ. Smith BM, et al. Among authors: covel ja. J Med Chem. 2008 Jan 24;51(2):305-13. doi: 10.1021/jm0709034. Epub 2007 Dec 21. J Med Chem. 2008. PMID: 18095642
A calcineurin antifungal strategy with analogs of FK506.
Nambu M, Covel JA, Kapoor M, Li X, Moloney MK, Numa MM, Soltow QA, Trzoss M, Webb P, Webb RR 2nd, Mutz M. Nambu M, et al. Among authors: covel ja. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2465-2471. doi: 10.1016/j.bmcl.2017.04.004. Epub 2017 Apr 3. Bioorg Med Chem Lett. 2017. PMID: 28412204
Total synthesis of bryostatin 1.
Keck GE, Poudel YB, Cummins TJ, Rudra A, Covel JA. Keck GE, et al. Among authors: covel ja. J Am Chem Soc. 2011 Feb 2;133(4):744-7. doi: 10.1021/ja110198y. Epub 2010 Dec 22. J Am Chem Soc. 2011. PMID: 21175177 Free PMC article.
13 results