5425-50-3Relevant articles and documents
Hydrazone derivatives enhance antileishmanial activity of thiochroman-4-ones
Vargas, Esteban,Echeverri, Fernando,Upegui, Yulieth A.,Robledo, Sara M.,Qui?ones, Wiston
, (2018/01/12)
Cutaneous leishmaniasis (CL) is a neglected tropical disease, which causes severe skin lesions. Due to the lack of effective vaccines, and toxicity or reduced effectiveness of available drugs in addition to complex and prolonged treatments, there is an urgent need to develop alternatives for the treatment for CL with 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 the intracellular amastigote form of Leishmania panamensis and cytotoxic activity against human monocytes (U-937 ATCC CRL-1593.2). Our results show that derivatization of the thiochroman-4-ones with acyl hydrazones significantly enhances the antileishmanial activity. Among the compounds tested semicarbazone and thiosemicarbazone derivatives of thioflavanone 19 and 20 displayed the highest antileishmanial activities, with EC50 values of 5.4 and 5.1 μM and low cytotoxicities (100.2 and 50.1 μM respectively), resulting in higher indexes of selectivity (IS).
Visible-Light-Driven Iron-Promoted Thiocarboxylation of Styrenes and Acrylates with CO2
Ye, Jian-Heng,Miao, Meng,Huang, He,Yan, Si-Shun,Yin, Zhu-Bao,Zhou, Wen-Jun,Yu, Da-Gang
supporting information, p. 15416 - 15420 (2017/11/01)
The first thiocarboxylation of styrenes and acrylates with CO2 was realized by using visible light as a driving force and catalytic iron salts as promoters. A variety of important β-thioacids were obtained in high yields. This multicomponent reaction proceeds in an atom- and redox-economical manner with broad substrate scope under mild reaction conditions. Notably, high regio-, chemo-, and diasteroselectivity are observed. Mechanistic studies indicate that a radical pathway can account for the unusual regioselectivity.
Fluoroboric acid adsorbed on silica-gel (HBF4-SiO2) as a new, highly efficient and reusable heterogeneous catalyst for thia-Michael addition to α,β-unsaturated carbonyl compounds
Sharma, Gaurav,Kumar, Raj,Chakraborti, Asit K.
, p. 4272 - 4275 (2008/09/21)
Fluoroboric acid adsorbed on silica-gel (HBF4-SiO2) has been found to be a new and highly efficient heterogeneous catalyst for thia-Michael addition to α,β-unsaturated carbonyl compounds under solvent-free conditions. In the case of
