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Vara Prasad, J.V. et al.

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties.

Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-SPh (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their antiviral activities. Both the enantiomers of inhibitor 15 were synthesized. The in vitro resistance profile, inhibitory activities against cytochrome P450 isozymes and pharmacokinetic properties of inhibitor 15S will be discussed.[1]

References

Nonpeptidic HIV protease inhibitors: 6-alkyl-5,6-dihydropyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl,5-methylphenyl thio) moiety: antiviral activities and pharmacokinetic properties. Vara Prasad, J.V., Boyer, F.E., Domagala, J.M., Ellsworth, E.L., Gajda, C., Hagen, S.E., Markoski, L.J., Tait, B.D., Lunney, E.A., Tummino, P.J., Ferguson, D., Holler, T., Hupe, D., Nouhan, C., Gracheck, S.J., VanderRoest, S., Saunders, J., Iyer, K., Sinz, M., Brodfuehrer, J. Bioorg. Med. Chem. Lett. (1999) [Pubmed]

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