Can I read 3-Hydroxy-2-methylene-3-(4-nitrophenylpropanenitrile): A new highly active compound against epimastigote and trypomastigote form of Trypanosoma cruzi on EtoBox?

3-Hydroxy-2-methylene-3-(4-nitrophenylpropanenitrile): A new highly active compound against epimastigote and trypomastigote form of Trypanosoma cruzi by Jana M. Sandes; Andrezza R. Borges; Cláudio G.L. Junior; Fábio P.L. Silva; Gabriel A.U. Carvalho; Gerd B. Rocha; Mário L.A.A. Vasconcellos; Regina C.B.Q. Figueiredo is a Chemistry article available to read on EtoBox.

What is 3-Hydroxy-2-methylene-3-(4-nitrophenylpropanenitrile): A new highly active compound against epimastigote and trypomastigote form of Trypanosoma cruzi about?

We have synthesized the Morita-Baylis-Hillman adduct (MBHA) 3-hydroxy-2-methylene-3-(4-nitrophenyl)-propanenitrile (3) in quantitative yield and evaluated on Trypanosoma cruzi epimastigote and bloodstream trypomastigote forms. Compound 3 strongly inhibited epimastigote growth, with IC 50 / 72 h of 28.5 lM and also caused intense trypomastigotes lysis, with an IC 50 /24 h of 25.5 lM. Ultrastructural analysis showed significant morphological changes on both parasite forms treated with 3, including increase of cell volume and rounding of cell body as well as intense intracellular disorganization. Morphological changes indicative of apoptosis, autophagy or necrosis were observed in most affected cells. Docking calculations of 1, 2 and 3 pointed out the possibility of T. cruzi Farnesyl Pyrophosphate Synthase (TcFPPS) enzyme inhibition in 3 mechanism of action.

Who reads 3-Hydroxy-2-methylene-3-(4-nitrophenylpropanenitrile): A new highly active compound against epimastigote and trypomastigote form of Trypanosoma cruzi?

Author

Jana M. Sandes; Andrezza R. Borges; Cláudio G.L. Junior; Fábio P.L. Silva; Gabriel A.U. Carvalho; Gerd B. Rocha; Mário L.A.A. Vasconcellos; Regina C.B.Q. Figueiredo

Publisher

Elsevier Science; Elsevier ; Elsevier Inc.; Elsevier BV (ISSN 0045-2068)

Published

2010

Language

EN

Field

Chemistry (Physical Sciences)