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Stereoisomers of ketoconazole: preparation and biological activity.
Rotstein DM, Kertesz DJ, Walker KA, Swinney DC. Rotstein DM, et al. J Med Chem. 1992 Jul 24;35(15):2818-25. doi: 10.1021/jm00093a015. J Med Chem. 1992. PMID: 1495014
Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.
Wanner J, Chen L, Lemoine RC, Kondru R, Jekle A, Heilek G, deRosier A, Ji C, Berry PW, Rotstein DM. Wanner J, et al. Among authors: rotstein dm. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6802-7. doi: 10.1016/j.bmcl.2010.08.118. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855212
Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.
Lemoine RC, Petersen AC, Setti L, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein DM. Lemoine RC, et al. Among authors: rotstein dm. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4753-6. doi: 10.1016/j.bmcl.2010.06.135. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20643548
Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.
Rotstein DM, Gabriel SD, Manser N, Filonova L, Padilla F, Sankuratri S, Ji C, deRosier A, Dioszegi M, Heilek G, Jekle A, Weller P, Berry P. Rotstein DM, et al. Bioorg Med Chem Lett. 2010 Jun 1;20(11):3219-22. doi: 10.1016/j.bmcl.2010.04.077. Epub 2010 Apr 22. Bioorg Med Chem Lett. 2010. PMID: 20457517
Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.
Rotstein DM, Melville CR, Padilla F, Cournoyer D, Lee EK, Lemoine R, Petersen AC, Setti LQ, Wanner J, Chen L, Filonova L, Loughhead DG, Manka J, Lin XF, Gleason S, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Mau CI, Weller P. Rotstein DM, et al. Bioorg Med Chem Lett. 2010 May 15;20(10):3116-9. doi: 10.1016/j.bmcl.2010.03.095. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20417098
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
Lemoine RC, Petersen AC, Setti L, Chen L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Rotstein DM. Lemoine RC, et al. Among authors: rotstein dm. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1830-3. doi: 10.1016/j.bmcl.2010.02.004. Epub 2010 Feb 6. Bioorg Med Chem Lett. 2010. PMID: 20176481
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.
Lemoine RC, Petersen AC, Setti L, Baldinger T, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Rotstein DM. Lemoine RC, et al. Among authors: rotstein dm. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1674-6. doi: 10.1016/j.bmcl.2010.01.080. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137937
Discovery of a potent, selective and orally bioavailable 3,9-diazaspiro[5.5]undeca-2-one CCR5 antagonist.
Yang H, Lin XF, Padilla F, Gabriel SD, Heilek G, Ji C, Sankuratri S, deRosier A, Berry P, Rotstein DM. Yang H, et al. Among authors: rotstein dm. Bioorg Med Chem Lett. 2009 Jan 1;19(1):209-13. doi: 10.1016/j.bmcl.2008.10.115. Epub 2008 Oct 31. Bioorg Med Chem Lett. 2009. PMID: 19014885
Spiropiperidine CCR5 antagonists.
Rotstein DM, Gabriel SD, Makra F, Filonova L, Gleason S, Brotherton-Pleiss C, Setti LQ, Trejo-Martin A, Lee EK, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Weller P, Mau CI. Rotstein DM, et al. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5401-6. doi: 10.1016/j.bmcl.2009.07.122. Epub 2009 Jul 30. Bioorg Med Chem Lett. 2009. PMID: 19674898
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.
Gong L, Han X, Silva T, Tan YC, Goyal B, Tivitmahaisoon P, Trejo A, Palmer W, Hogg H, Jahagir A, Alam M, Wagner P, Stein K, Filonova L, Loe B, Makra F, Rotstein D, Rapatova L, Dunn J, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Hermann J, Kuglstatter A, Goldstein D. Gong L, et al. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3565-9. doi: 10.1016/j.bmcl.2013.04.029. Epub 2013 Apr 21. Bioorg Med Chem Lett. 2013. PMID: 23664880
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