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

New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.

On the basis of previously described X-ray studies of an enzyme/aza-dipeptide complex,8 aza-dipeptide analogues carrying N-(bis-aryl-methyl) substituents on the (hydroxethyl)hydrazine moiety have been designed and synthesized as HIV-1 protease inhibitors. By using either equally (12) or orthogonally (13) protected dipeptide isosteres, symmetrically and asymmetrically acylated aza-dipeptides can be synthesized. This approach led to the discovery of very potent inhibitors with antiviral activities (ED50) in the subnanomolar range. Acylation of the (hydroxethyl)hydrazine dipeptide isostere with the L-tert-leucine derivative 29 increased the oral bioavailability significantly when compared to the corresponding L-valine or L-isoleucine derivatives. The bis(L-tert-leucine) derivatives CGP 75355, CGP 73547, CGP 75136, and CGP 75176 combine excellent antiviral activity with high blood concentration after oral administration. Furthermore, they show no cross-resistance with saquinavir-resistant strains and maintain activity against indinavir-resistant ones. Consequently they qualify for further profiling as potential clinical candidates.[1]


  1. New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development. Bold, G., Fässler, A., Capraro, H.G., Cozens, R., Klimkait, T., Lazdins, J., Mestan, J., Poncioni, B., Rösel, J., Stover, D., Tintelnot-Blomley, M., Acemoglu, F., Beck, W., Boss, E., Eschbach, M., Hürlimann, T., Masso, E., Roussel, S., Ucci-Stoll, K., Wyss, D., Lang, M. J. Med. Chem. (1998) [Pubmed]
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