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A series of twelve substituted 2‐phenylquinoline‐4‐carboxylic acids analogous to antimalarial and antileishmanial natural products was developed via the Döbner reaction employing microwave irradiation (MW). The products were obtained in moderate yields in 0.5‐3 minutes and nine of them were evaluated in vitro against the parasites responsible for malaria, leishmaniasis and trypanosomiasis diseases (WHO, Switzerland). Four compounds exhibited activity against Trypanosoma cruzi and another two resulted active against Plasmodium falciparum and Leishmania infantum, respectively.

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Microwave solvent-free reaction conditions are explored to prepare quinoline derivatives with antiparasitic activity. Preliminary tests of some products reveal generally moderate effects. The piperidinyl derivative (VII) is found to be almost as active for Chagas' disease as the reference standard benznidazole. -(MUSCIA, G. C.; BOLLINI, M.; CARNEVALE, J. P.; BRUNO, A. M.; ASIS*, S. E.; Tetrahedron Lett. 47 (2006) 50, 8811-8815; Dep. Quim. Org., Fac. Farm.

is synthesized by microwave-assisted one-pot reaction of pyruvic acid with anilines and benzaldehydes. Some of the title compounds show antiparasitic activities but their IC50 values are quite far from the reference drugs. -(MUSCIA, G. C.; CARNEVALE, J. P.; BOLLINI, M.; ASIS*, S. E.; J. Heterocycl. Chem. 45 (2008) 2, 611-614; Dep. Quim. Org., Fac. Farm. Bioquim., Univ. Buenos Aires, 1113 Buenos Aires, Argent.; Eng.) -H. Toeppel 29-145