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Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family.
McCombie SW, Lin SI, Tagat JR, Nazareno D, Vice S, Ford J, Asberom T, Leone D, Kozlowski JA, Zhou G, Ruperto VB, Duffy RA, Lachowicz JE. McCombie SW, et al. Among authors: lachowicz je. Bioorg Med Chem Lett. 2002 Mar 11;12(5):795-8. doi: 10.1016/s0960-894x(02)00024-0. Bioorg Med Chem Lett. 2002. PMID: 11859005
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. J Med Chem. 2004 May 6;47(10):2405-8. doi: 10.1021/jm0304515. J Med Chem. 2004. PMID: 15115380
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: lachowicz je. 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: lachowicz je. 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
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H 3rd, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE. Wang Y, et al. Among authors: lachowicz je. J Med Chem. 2002 Dec 5;45(25):5415-8. doi: 10.1021/jm0255163. J Med Chem. 2002. PMID: 12459007
Cyclobutane derivatives as potent NK1 selective antagonists.
Wrobleski ML, Reichard GA, Paliwal S, Shah S, Tsui HC, Duffy RA, Lachowicz JE, Morgan CA, Varty GB, Shih NY. Wrobleski ML, et al. Among authors: lachowicz je. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3859-63. doi: 10.1016/j.bmcl.2006.04.031. Epub 2006 May 8. Bioorg Med Chem Lett. 2006. PMID: 16682196
78 results