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If you liked this document, tag it with the WordPress tag: No tags for this post.Synthesis and evaluation of a novel class of synthetic saquinavir derivatives as anti-AIDS drugs.
Twenty five saquinavir derivatives with various functionalities were prepared and screened for antiviral activity. Among them, N-3-[4-(1,1-dimethylethyl)-phenyl]-2-(3-oxo-4-thia-1-azabicyclo[2.2.1]heptyl) pyrrolidine-1-carboxamide (24) displayed significant anti-HIV activity, with EC(50) of 3.8 microg/mL, ID(50) of 16.5 microg/mL, SI(50) of 20.8 and CC(50) of 290.4 microg/mL. Compound 24 was more active than indinavir and zidovudine, but not active as ritonavir. The antiviral activity was found to be dependent on the hydrophobic chain length of the lipophilic substituents of the pyrrolidine moiety.
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