Piperazine-Based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element

Autor: Tagat, J. R., McCombie, S. W., Steensma, R. W., Lin, S. I., Nazareno, D. V., Baroudy, B., Vantuno, N., Xu, S., Liu, J.

Publikováno v: Bioorganic & Medicinal Chemistry Letters; 2001, Vol. 11 Issue: 16 p2143-2146, 4p

Synthetic Inhibitors of Interleukin-6 I: 2,3,7,8-Tetrahydro-4-Aryl-1H-Cyclopent [e] Imidazo [L,2-a]- Pyridin-5(6h)-One and Related Compounds

Autor: Tagat, J. R., Nazareno, D. V., McCombie, S. W., Barton, B. E.

Publikováno v: Bioorganic & Medicinal Chemistry Letters; 1995, Vol. 5 Issue: 18 p2139-2139, 1p

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.

Autor: Tagat JR; Departments of Chemical Research, Drug Metabolism & Pharmacokinetics, and Antiviral Therapy, Schering-Plough Research Institute, K-15-2B-2800, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA. jayaram.tagat@spcorp.com, Steensma RW, McCombie SW, Nazareno DV, Lin SI, Neustadt BR, Cox K, Xu S, Wojcik L, Murray MG, Vantuno N, Baroudy BM, Strizki JM

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2001 Oct 11; Vol. 44 (21), pp. 3343-6.