Antimalarial Activity of 4‐(5‐Trifluoromethyl‐1H‐pyrazol‐1‐yl)chloroquine Analogues.

Abstract

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

β-Alkoxyvinyl trifluoromethyl ketones as efficient precursors for the one-pot synthesis of bis-(4,5-dihydro-1H-pyrazol-1-yl)methanones and 1H-pyrazolyl-1-carbohydrazides

“…In particular, the synthetic potential of β-alkoxyvinyl trifluoromethyl ketones to obtain a series of novel trifluoromethylated pyrazoles has recently been explored and their biological evaluation reported by us. 10,13,[21][22][23] The reactions of 4-alkoxy-4-aryl(heteroaryl)-1,1,1-trifluoro-3-alken-2-ones (1b-e,1h-i) with carbohydrazide were carried out in 1:1 molar ratio in ethanol, and all reactions were monitored by TLC. The most satisfactory results were obtained when the reactions were performed under mild conditions.…”

1-[({5-[(4-Methylphenoxy)methyl]-4-phenyl-4H-1,2,4-triazol-3-yl}sulfanyl)methyl]-1H-benzo[d][1,2,3]triazole

“…Triazole-based drugs such as fluconazole, ketoconazole, itraconazole, voriconazole, ravuconazole and posaconazole have shown remarkable anti-fungal activities (Sheehan et al, 1999;Sü kü roglu et al, 2005;Bekhit et al, 2005;Cunico et al, 2006). In this context we report herein the synthesis and crystal structure of the title compound.…”

Screening of some pyrazole derivatives as promising antileishmanial agent

“…Pyrazole derivatives were found to possess various important biological activities, such as antibacterial (Samir et al, 2011;Nilesh and Manish, 2011), antiinflammatory (Adnan et al, 2008;Lingaiah et al, 2011), antioxidant (Ramesh and Chetan, 2011) ACE inhibitory (Marco et al, 2010), anti-cancer (Hai-Jun et al, 2010, MAO-B inhibitory (Nesrin et al, 2007), antidepressant (Mohamed et al, 2009), antiviral (Guiping et al, 2008), antimycobacterial (Ramaiyan et al, 2010;Daniele et al, 2008), antileishmanial (Bernardino et al, 2006;Naresh et al, 2006), and antimalarial (Katiyar et al, 2005;Cunico et al, 2006) activities.…”