Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones

• DOI: 10.20944/preprints201711.0177.v1
• Publication Date: 2017-11-29T04:38:11Z
• Authors: Esteban Vargas; Fernando Echeverri; Yulieth A. Upegui; Sara M. Robledo; Wiston Quiñones
• Keywords: Amastigote; Hydrazone; Semicarbazone; IC50; EC50

Cutaneous Leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, treatment can be complex and prolonged, high toxicity, side effects cost, there an urgent need develop alternatives for CL that may have different mechanisms action. In our effort search new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives thiochroman-4-ones. Compounds were evaluated their in vitro antileishmanial activity intracellular amastigotes form panamensis cytotoxic human monocytes (U-937 ATCC CRL-1593.2); results show derivatization with hydrazones significantly enhance activity, among compounds tested semicarbazone (19) thiosemicarbazone (20) thioflavanone display highest activities EC50 values 5.4 5.1 µM both low cytotoxicities, 100.2 50.1 resulting selectivity index (SI).