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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: beaton g. 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: beaton g. 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
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia.
Lavrador-Erb K, Ravula SB, Yu J, Zamani-Kord S, Moree WJ, Petroski RE, Wen J, Malany S, Hoare SR, Madan A, Crowe PD, Beaton G. Lavrador-Erb K, et al. Among authors: beaton g. Bioorg Med Chem Lett. 2010 May 1;20(9):2916-9. doi: 10.1016/j.bmcl.2010.03.027. Epub 2010 Mar 10. Bioorg Med Chem Lett. 2010. PMID: 20347297
Selectivity profiling of novel indene H(1)-antihistamines for the treatment of insomnia.
Li BF, Moree WJ, Yu J, Coon T, Zamani-Kord S, Malany S, Jalali K, Wen J, Wang H, Yang C, Hoare SR, Petroski RE, Madan A, Crowe PD, Beaton G. Li BF, et al. Among authors: beaton g. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2629-33. doi: 10.1016/j.bmcl.2010.02.055. Epub 2010 Feb 18. Bioorg Med Chem Lett. 2010. PMID: 20227880
Novel benzothiophene H1-antihistamines for the treatment of insomnia.
Moree WJ, Jovic F, Coon T, Yu J, Li BF, Tucci FC, Marinkovic D, Gross RS, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G. Moree WJ, et al. Among authors: beaton g. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2316-20. doi: 10.1016/j.bmcl.2010.01.134. Epub 2010 Feb 2. Bioorg Med Chem Lett. 2010. PMID: 20188547
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Moree WJ, Li BF, Jovic F, Coon T, Yu J, Gross RS, Tucci F, Marinkovic D, Zamani-Kord S, Malany S, Bradbury MJ, Hernandez LM, O'Brien Z, Wen J, Wang H, Hoare SR, Petroski RE, Sacaan A, Madan A, Crowe PD, Beaton G. Moree WJ, et al. Among authors: beaton g. J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k. J Med Chem. 2009. PMID: 19663387
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.
Coon T, Moree WJ, Li B, Yu J, Zamani-Kord S, Malany S, Santos MA, Hernandez LM, Petroski RE, Sun A, Wen J, Sullivan S, Haelewyn J, Hedrick M, Hoare SJ, Bradbury MJ, Crowe PD, Beaton G. Coon T, et al. Among authors: beaton g. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4380-4. doi: 10.1016/j.bmcl.2009.05.086. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19553115
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