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Page 1
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
Kozlowski JA, Zhou G, Tagat JR, Lin SI, McCombie SW, Ruperto VB, Duffy RA, McQuade RA, Crosby G, Taylor LA, Billard W, Binch H, Lachowicz JE. Kozlowski JA, et al. Among authors: mccombie sw. Bioorg Med Chem Lett. 2002 Mar 11;12(5):791-4. doi: 10.1016/s0960-894x(02)00023-9. Bioorg Med Chem Lett. 2002. PMID: 11859004
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H 3rd, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: mccombie sw. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3479-82. doi: 10.1016/s0960-894x(02)00742-4. Bioorg Med Chem Lett. 2002. PMID: 12419388
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagonist.
Tagat JR, McCombie SW, Nazareno D, Labroli MA, Xiao Y, Steensma RW, Strizki JM, Baroudy BM, Cox K, Lachowicz J, Varty G, Watkins R. Tagat JR, et al. Among authors: mccombie sw. J Med Chem. 2004 May 6;47(10):2405-8. doi: 10.1021/jm0304515. J Med Chem. 2004. PMID: 15115380
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Lavey BJ, Kozlowski JA, Shankar BB, Spitler JM, Zhou G, Yang DY, Shu Y, Wong MK, Wong SC, Shih NY, Wu J, McCombie SW, Rizvi R, Wolin RL, Lunn CA. Lavey BJ, et al. Among authors: mccombie sw. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3760-4. doi: 10.1016/j.bmcl.2007.04.028. Epub 2007 Apr 10. Bioorg Med Chem Lett. 2007. PMID: 17466519
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Boyle CD, Chackalamannil S, Clader JW, Greenlee WJ, Josien HB, Kaminski JJ, Kozlowski JA, McCombie SW, Nazareno DV, Tagat JR, Wang Y, Zhou G, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: mccombie sw. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2311-4. doi: 10.1016/s0960-894x(01)00435-8. Bioorg Med Chem Lett. 2001. PMID: 11527721
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Tagat JR, Steensma RW, McCombie SW, Nazareno DV, Lin SI, Neustadt BR, Cox K, Xu S, Wojcik L, Murray MG, Vantuno N, Baroudy BM, Strizki JM. Tagat JR, et al. Among authors: mccombie sw. J Med Chem. 2001 Oct 11;44(21):3343-6. doi: 10.1021/jm0155401. J Med Chem. 2001. PMID: 11585438
30 results