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Figure 3. Comparison of the inhibition of the protein farnesylation with
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new chemotherapeutics for the treatment of malaria. In
comparison to previously described compounds, our farnesyl-
transferase inhibitors based on the benzophenone scaffold
possess superior activity. To the best of our knowledge, we
have demonstrated for the first time an in vivo activity of
farnesyltransferase inhibitors against plasmodium infections.
The future development of this class of compounds will
primarily be aimed at achieving oral bioavailability and
further increasing the activity.
Received: February 13, 2003
Revised: September 12, 2003 [Z51169]
Keywords: drug design · enzyme inhibitors · farnesyltransferase ·
.
malaria · medicinal chemistry
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