Indinavir structure-based design

Finally, Samuelsson and co-workers designed a new C2-symmetric HIV-PR inhibitor, on the basis of X-ray crystal structures, which indicated that the HIV protease existed as a C2-symmetric dimer. The peptidomimetic scaffold of this new class of inhibitors was based on D-mannitol and duplication of the C-terminus. Compounds 21 and 22 were rapidly synthesized and displayed comparable enzyme-inhibitory and antiviral potencies to Indinavir (Figure 24.4, Table 24.1).29-32... 

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