Synthesis and biological evaluation of some novel 1-indanone thiazolylhydrazone derivatives as anti-Trypanosoma cruzi agents

QSAR study and conformational analysis of 4-arylthiazolylhydrazones derived from 1-indanones with anti-Trypanosoma cruzi activity

“…The synthetic pathway for the preparation of the new TZHs 18-20 (depicted in Scheme 1) is based on the method previously described by us for the synthesis of TZHs 1-17 (Caputto et al, 2012). The new compounds were obtained from the reaction of the thiosemicarbazone of 1-indanones conveniently substituted and the corresponding phenacyl halides.…”

“…4-Methoxyphenacyl bromide and 4-nitro-phenacyl bromide were purchased from Sigma-Aldrich and used as received. 4-Fluor-phenacyl chloride and thiosemicarbazones derived from 1-indanones were prepared according to the protocols previously described (Caputto et al, 2012(Caputto et al, , 2011Finkielsztein et al, 2008).…”

“…Most of these new derivatives exhibited promising activity against the different forms of T. cruzi and were more potent and selective than the reference drug benznidazole (Caputto et al, 2012). A preliminary analysis of the structure-activity relationship suggested that better trypanocidal activity may be attained when R 1 , R 2 or R 3 is a methyl group (Fig.…”

Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones

“…Structures of thiochroman-4-ones ( [1][2][3][4][5] and hydrazone derivatives (6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22). …”

“…In addition, numerous hydrazones have been reported to possess interesting biological activities such as antitumoral, antiviral and antiparasitic effects [8][9][10]; some hydrazones also exhibit activity against the parasites that cause malaria, leishmaniasis and Chagas disease [3,[11][12][13][14][15][16][17][18], where the inhibition of proteases and represent the most common mechanism of action for the hydrazones [16,[19][20][21].…”