Article
Version 1
Preserved in Portico This version is not peer-reviewed
Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones
Version 1
: Received: 27 November 2017 / Approved: 27 November 2017 / Online: 27 November 2017 (09:35:23 CET)
Version 2 : Received: 29 December 2017 / Approved: 2 January 2018 / Online: 2 January 2018 (10:11:55 CET)
Version 2 : Received: 29 December 2017 / Approved: 2 January 2018 / Online: 2 January 2018 (10:11:55 CET)
A peer-reviewed article of this Preprint also exists.
Vargas, E.; Echeverri, F.; Upegui, Y.A.; Robledo, S.M.; Quiñones, W. Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones. Molecules 2018, 23, 70. Vargas, E.; Echeverri, F.; Upegui, Y.A.; Robledo, S.M.; Quiñones, W. Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones. Molecules 2018, 23, 70.
Abstract
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 and high cost, there is an urgent need to develop alternatives for the treatment for CL that may have different mechanisms of action. In our effort to search for new promising hits against Leishmania parasites we prepared 18 acyl hydrazone derivatives of thiochroman-4-ones. Compounds were evaluated for their in vitro antileishmanial activity against intracellular amastigotes form of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2); our results show that derivatization with acyl hydrazones significantly enhance the antileishmanial activity, among the compounds tested semicarbazone (19) and thiosemicarbazone (20) derivatives of thioflavanone display the highest antileishmanial activities with EC50 values of 5.4 and 5.1 µM both with low cytotoxicities, 100.2 a 50.1 µM resulting in high selectivity index (SI).
Keywords
Leishmania; thiochroman-4-ones; acyl hydrazone; cytotoxicity
Subject
Chemistry and Materials Science, Medicinal Chemistry
Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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