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Page 1
Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D. Chen C, et al. Among authors: hoare sr. Bioorg Med Chem. 2008 May 15;16(10):5606-18. doi: 10.1016/j.bmc.2008.03.072. Epub 2008 Apr 1. Bioorg Med Chem. 2008. PMID: 18417348
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Moree WJ, Li BF, Zamani-Kord S, Yu J, Coon T, Huang C, Marinkovic D, Tucci FC, Malany S, Bradbury MJ, Hernandez LM, Wen J, Wang H, Hoare SR, Petroski RE, Jalali K, Yang C, Sacaan A, Madan A, Crowe PD, Beaton G. Moree WJ, et al. Among authors: hoare sr. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5874-8. doi: 10.1016/j.bmcl.2010.07.117. Epub 2010 Aug 3. Bioorg Med Chem Lett. 2010. PMID: 20800486
Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H₁-antihistamines for insomnia.
Ravula SB, Yu J, Tran JA, Arellano M, Tucci FC, Moree WJ, Li BF, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G. Ravula SB, et al. Among authors: hoare sr. Bioorg Med Chem Lett. 2012 Jan 1;22(1):421-6. doi: 10.1016/j.bmcl.2011.10.115. Epub 2011 Nov 15. Bioorg Med Chem Lett. 2012. PMID: 22153347
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
Tran JA, Tucci FC, Jiang W, Marinkovic D, Chen CW, Arellano M, Markison S, Fleck BA, Wen J, White NS, Pontillo J, Saunders J, Marks D, Hoare SR, Madan A, Foster AC, Chen C. Tran JA, et al. Among authors: hoare sr. Bioorg Med Chem. 2007 Aug 1;15(15):5166-76. doi: 10.1016/j.bmc.2007.05.026. Epub 2007 May 17. Bioorg Med Chem. 2007. PMID: 17544282
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Jiang W, Tucci FC, Tran JA, Fleck BA, Wen J, Markison S, Marinkovic D, Chen CW, Arellano M, Hoare SR, Johns M, Foster AC, Saunders J, Chen C. Jiang W, et al. Among authors: hoare sr. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5610-3. doi: 10.1016/j.bmcl.2007.07.097. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17822895
Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen C, Jiang W, Tucci F, Tran JA, Fleck BA, Hoare SR, Joppa M, Markison S, Wen J, Sai Y, Johns M, Madan A, Chen T, Chen CW, Marinkovic D, Arellano M, Saunders J, Foster AC. Chen C, et al. Among authors: hoare sr. J Med Chem. 2007 Nov 1;50(22):5249-52. doi: 10.1021/jm070806a. Epub 2007 Oct 5. J Med Chem. 2007. PMID: 17918824
Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Tran JA, Jiang W, Tucci FC, Fleck BA, Wen J, Sai Y, Madan A, Chen TK, Markison S, Foster AC, Hoare SR, Marks D, Harman J, Chen CW, Arellano M, Marinkovic D, Bozigian H, Saunders J, Chen C. Tran JA, et al. Among authors: hoare sr. J Med Chem. 2007 Dec 13;50(25):6356-66. doi: 10.1021/jm701137s. Epub 2007 Nov 10. J Med Chem. 2007. PMID: 17994683
Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Chen C, Jiang W, Tran JA, Tucci FC, Fleck BA, Markison S, Wen J, Madan A, Hoare SR, Foster AC, Marinkovic D, Chen CW, Arellano M, Saunders J. Chen C, et al. Among authors: hoare sr. Bioorg Med Chem Lett. 2008 Jan 1;18(1):129-36. doi: 10.1016/j.bmcl.2007.10.115. Epub 2007 Nov 4. Bioorg Med Chem Lett. 2008. PMID: 18032040
118 results