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(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
Mullen G, Napier J, Balestra M, DeCory T, Hale G, Macor J, Mack R, Loch J 3rd, Wu E, Kover A, Verhoest P, Sampognaro A, Phillips E, Zhu Y, Murray R, Griffith R, Blosser J, Gurley D, Machulskis A, Zongrone J, Rosen A, Gordon J. Mullen G, et al. Among authors: loch j 3rd. J Med Chem. 2000 Nov 2;43(22):4045-50. doi: 10.1021/jm000249r. J Med Chem. 2000. PMID: 11063601
In vitro muscarinic activity of spiromuscarones and related analogs.
Wu ES, Griffith RC, Loch JT 3rd, Kover A, Murray RJ, Mullen GB, Blosser JC, Machulskis AC, McCreedy SA. Wu ES, et al. Among authors: loch jt 3rd. J Med Chem. 1995 Apr 28;38(9):1558-70. doi: 10.1021/jm00009a016. J Med Chem. 1995. PMID: 7739014
Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.
Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, DeGrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE. Sherer BA, et al. Among authors: loch jt 3rd. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7416-20. doi: 10.1016/j.bmcl.2011.10.010. Epub 2011 Oct 12. Bioorg Med Chem Lett. 2011. PMID: 22041057
Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.
Murphy-Benenato KE, Gingipalli L, Boriack-Sjodin PA, Martinez-Botella G, Carcanague D, Eyermann CJ, Gowravaram M, Harang J, Hale MR, Ioannidis G, Jahic H, Johnstone M, Kutschke A, Laganas VA, Loch JT 3rd, Miller MD, Oguto H, Patel SJ. Murphy-Benenato KE, et al. Among authors: loch jt 3rd. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5172-7. doi: 10.1016/j.bmcl.2015.09.075. Epub 2015 Oct 14. Bioorg Med Chem Lett. 2015. PMID: 26463129
Pyrrolamide DNA gyrase inhibitors: fragment-based nuclear magnetic resonance screening to identify antibacterial agents.
Eakin AE, Green O, Hales N, Walkup GK, Bist S, Singh A, Mullen G, Bryant J, Embrey K, Gao N, Breeze A, Timms D, Andrews B, Uria-Nickelsen M, Demeritt J, Loch JT 3rd, Hull K, Blodgett A, Illingworth RN, Prince B, Boriack-Sjodin PA, Hauck S, MacPherson LJ, Ni H, Sherer B. Eakin AE, et al. Among authors: loch jt 3rd. Antimicrob Agents Chemother. 2012 Mar;56(3):1240-6. doi: 10.1128/AAC.05485-11. Epub 2011 Dec 19. Antimicrob Agents Chemother. 2012. PMID: 22183167 Free PMC article.
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA. Martínez-Botella G, et al. Among authors: loch jt. J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23043329
91 results