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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Tagat, J.R. et al.

Tagat, Steensma, McCombie, Nazareno, Lin, Neustadt, Cox, Xu, Wojcik, Murray, Vantuno, Baroudy, Strizki,

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.

Truncation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. Further optimization for pharmacokinetic properties afforded Sch-350634 (1), a prototypical piperazine-based CCR5 antagonist, which is a potent inhibitor of HIV-1 entry and replication in PBMCs. The title compound (1) has excellent oral bioavailability in rat, dog, and monkey.[1]

References

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, J.R., Steensma, R.W., McCombie, S.W., Nazareno, D.V., Lin, S.I., Neustadt, B.R., Cox, K., Xu, S., Wojcik, L., Murray, M.G., Vantuno, N., Baroudy, B.M., Strizki, J.M. J. Med. Chem. (2001) [Pubmed]

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