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Page 1
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: petroski re. 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
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: petroski re. J Med Chem. 2009 Sep 10;52(17):5307-10. doi: 10.1021/jm900933k. J Med Chem. 2009. PMID: 19663387
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: petroski re. 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
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: petroski re. 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
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: petroski re. 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
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: petroski re. 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
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: petroski re. 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
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Rowbottom MW, Vickers TD, Dyck B, Grey J, Tamiya J, Zhang M, Kiankarimi M, Wu D, Dwight W, Wade WS, Schwarz D, Heise CE, Madan A, Fisher A, Petroski R, Goodfellow VS. Rowbottom MW, et al. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16814542
2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.
Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J. Slee DH, et al. J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29. J Med Chem. 2008. PMID: 18307293
Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.
Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH. Zhang X, et al. J Med Chem. 2008 Nov 27;51(22):7099-110. doi: 10.1021/jm800851u. J Med Chem. 2008. PMID: 18947224
30 results