We have demonstrated that the p-trifluoromethylphenylpropionylamino residue at the 2-position of the core structure leads to an active benzophenone-type anti-malarial agent. The attempt to improve water solubility by introduction of an amino group into the alpha-position of the arylpropionyl residue resulted in decreased activity.
Acid Amides. -Replacement of the 2-arylacetylamino residue, attached to the diaminobenzophenone scaffold of initial developed farnesyltransferase inhibitors, by several arylpropionyl residues leads to an active benzophenone-type anti-malarial agent, para trifluoromethyl derivative (VIc). Unfortunately, attempts to improve water solubility by introduction of an amino group into the α-position of the arylpropionyl residue are accompanied by a decrease of activity. -(WIESNER, J.; FUCIK, K.; KETTLER, K.; SAKOWSKI, J.; ORTMANN, R.; JOMAA, H.; SCHLITZER*, M.; Bioorg. Med. Chem. Lett. 13 (2003) 9, 1539-1541; Inst. Pharm., Zent. Pharmaforsch.,
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