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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. Among authors: heilek g. 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
Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.
Lemoine RC, Petersen AC, Setti L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein D. Lemoine RC, et al. Among authors: heilek g. Bioorg Med Chem Lett. 2010 Jan 15;20(2):704-8. doi: 10.1016/j.bmcl.2009.11.072. Epub 2009 Dec 7. Bioorg Med Chem Lett. 2010. PMID: 20004099
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. Among authors: heilek g. 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 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: heilek g. 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
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
Kertesz DJ, Brotherton-Pleiss C, Yang M, Wang Z, Lin X, Qiu Z, Hirschfeld DR, Gleason S, Mirzadegan T, Dunten PW, Harris SF, Villaseñor AG, Hang JQ, Heilek GM, Klumpp K. Kertesz DJ, et al. Among authors: heilek gm. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4215-8. doi: 10.1016/j.bmcl.2010.05.040. Epub 2010 May 16. Bioorg Med Chem Lett. 2010. PMID: 20538456
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