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The efficient multicomponent synthesis of thiazolidinones from the reaction of arenealdehydes, mercaptoacetic acid and 2-picolilamine or 2-aminopyridine under ultrasound irradiation are reported. The reaction with 2-aminopyridine needs a Lewis acid catalysis to afford the corresponding 2-aryl-3-(pyridin-2-yl)-1,3-thiazolidin-4-ones. All novel compounds were identified and characterized by (1)H and (13)C NMR spectra. Applying the sonochemical methodology, two series of heterocyclic thiazolidinones were synthesized in good yields after short reaction times.

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Quinoline derivatives R 0410Antimalarial Activity of 4-(5-Trifluoromethyl-1H-pyrazol-1-yl)chloroquine Analogues. -Compounds (VI) show in vitro antimalarial activity with (VIa) being the most active derivative (IC50 = 1.39 µg/ml). Aromatic compounds (VII) reveal a sharp decrease in activity. In vivo tests against NK-65 strain of P. berghei in infected mice lead to the result that (VIa) is inactive, while derivatives (VIb) and (VIc) show no loss of activity. -(CUNICO, W.; CECHINEL, C. A.; BONACORSO, H. G.; MARTINS, M. A. P.; ZANATTA, N.; DE SOUZA, M. V. N.; FREITAS, I. O.; SOARES, R. P. P.; KRETTLI*, A. U.; Bioorg. Med. Chem. Lett. 16 (2006) 3, 649-653; Dep. Parasitol., Univ. Fed. Minas Gerais, 30180 Belo Horizonte, Minas Gerais, Brazil; Eng.) -C. Oppel 18-137

The alternative synthesis of 12 1,2,4-oxadiazoles using ultrasound irradiation from trichloroacetoamidoxime and acyl chlorides is reported. Seven of them are novel compounds. The 3-trichloromethyl-5alkyl(aryl)-1,2,4-oxadiazoles have been synthesised in better yields and shorter reaction times compared to the conventional method. This protocol can be applicable for preparation of 1,2,4-oxadiazoles containing aryl or alkyl groups attached at their C-5 side-chain.