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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: strizki jm. J Med Chem. 2001 Oct 11;44(21):3343-6. doi: 10.1021/jm0155401. J Med Chem. 2001. PMID: 11585438
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: strizki jm. J Med Chem. 2004 May 6;47(10):2405-8. doi: 10.1021/jm0304515. J Med Chem. 2004. PMID: 15115380
Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.
Strizki JM, Tremblay C, Xu S, Wojcik L, Wagner N, Gonsiorek W, Hipkin RW, Chou CC, Pugliese-Sivo C, Xiao Y, Tagat JR, Cox K, Priestley T, Sorota S, Huang W, Hirsch M, Reyes GR, Baroudy BM. Strizki JM, et al. Antimicrob Agents Chemother. 2005 Dec;49(12):4911-9. doi: 10.1128/AAC.49.12.4911-4919.2005. Antimicrob Agents Chemother. 2005. PMID: 16304152 Free PMC article.
SCH-C (SCH 351125), an orally bioavailable, small molecule antagonist of the chemokine receptor CCR5, is a potent inhibitor of HIV-1 infection in vitro and in vivo.
Strizki JM, Xu S, Wagner NE, Wojcik L, Liu J, Hou Y, Endres M, Palani A, Shapiro S, Clader JW, Greenlee WJ, Tagat JR, McCombie S, Cox K, Fawzi AB, Chou CC, Pugliese-Sivo C, Davies L, Moreno ME, Ho DD, Trkola A, Stoddart CA, Moore JP, Reyes GR, Baroudy BM. Strizki JM, et al. Proc Natl Acad Sci U S A. 2001 Oct 23;98(22):12718-23. doi: 10.1073/pnas.221375398. Epub 2001 Oct 16. Proc Natl Acad Sci U S A. 2001. PMID: 11606733 Free PMC article.
49 results