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Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.
Liu KK, Lefker BA, Dombroski MA, Chiang P, Cornelius P, Patterson TA, Zeng Y, Santucci S, Tomlinson E, Gibbons CP, Marala R, Brown JA, Kong JX, Lee E, Werner W, Wenzel Z, Giragossian C, Chen H, Coffey SB. Liu KK, et al. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2365-9. doi: 10.1016/j.bmcl.2010.01.107. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20202843
Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.
Guzman-Perez A, Wester RT, Allen MC, Brown JA, Buchholz AR, Cook ER, Day WW, Hamanaka ES, Kennedy SP, Knight DR, Kowalczyk PJ, Marala RB, Mularski CJ, Novomisle WA, Ruggeri RB, Tracey WR, Hill RJ. Guzman-Perez A, et al. Among authors: brown ja. Bioorg Med Chem Lett. 2001 Mar 26;11(6):803-7. doi: 10.1016/s0960-894x(01)00059-2. Bioorg Med Chem Lett. 2001. PMID: 11277524
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Among authors: brown j. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
Filipski KJ, Bian J, Ebner DC, Lee EC, Li JC, Sammons MF, Wright SW, Stevens BD, Didiuk MT, Tu M, Perreault C, Brown J, Atkinson K, Tan B, Salatto CT, Litchfield J, Pfefferkorn JA, Guzman-Perez A. Filipski KJ, et al. Among authors: brown j. Bioorg Med Chem Lett. 2012 Jan 1;22(1):415-20. doi: 10.1016/j.bmcl.2011.10.113. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22119466
Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, Tu M, Stevens BD, Bian J, Aspnes G, Perreault C, Sammons MF, Wright SW, Litchfield J, Kalgutkar AS, Sharma R, Didiuk MT, Ebner DC, Filipski KJ, Brown J, Atkinson K, Pfefferkorn JA, Guzman-Perez A. Lee EC, et al. Among authors: brown j. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. doi: 10.1016/j.bmcl.2013.12.090. Epub 2013 Dec 28. Bioorg Med Chem Lett. 2014. PMID: 24418771
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