7‐Chloro‐4‐quinolinyl Hydrazones: A Promising and Potent Class of Antileishmanial Compounds

Abstract

In this work, we report the antileishmanial evaluation of twenty 7-chloro-4-quinolinyl hydrazone derivatives (1-20). Firstly, the compounds were tested against promastigotes of four different Leishmania species. After that, all derivatives were assayed against L. braziliensis amastigotes and murine macrophages. Furthermore, it was investigated whether the antiamastigote L. braziliensis effect of the compounds could be associated with nitric oxide production. Compounds 6 and 7 showed a strong leishmanicidal activity against intracellular parasite with IC50 in nanogram levels (30 and 20 ng/mL, respectively). Appreciable activity of three compounds tested can be considered an important finding for the rational design of new leads for antileishmanial compounds.

Synthesis, antileishmanial activity and QSAR studies of 2-chloro- N -arylacetamides

“…Therefore, the search for new cheap, potent and safe therapeutic alternatives is needed and has been pursued by several groups (Birhan, Bekhit, Hymete, 2014;Coimbra et al, 2013;Gómez-Pérez et al, 2014;Bonano et al, 2014;Gellis et al, 2012;Machado et al, 2012).…”

HPLC-DAD Analysis, Antileishmanial, Antiproliferative, and Antibacterial Activities ofLacistema pubescens: An Amazonian Medicinal Plant

“…Compounds with selectivity index (SI) ≥ 1.0 were considered more destructive to amastigotes of L. amazonensis than to the host cells [30]. Regarding to the selectivity of the samples, it is important to be mentioned that, despite the cytotoxic effect on macrophages, methanolic extract and hexane fraction were 4.1 and 3.6 times, respectively, more destructive to amastigote than to the host cells (Table 2).…”

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].…”