Design, Synthesis, Biological Evaluation and Molecular Modeling Studies of Novel Eugenol Esters as Leishmanicidal Agents
Author(s) -
Camila Coelho,
Thiago dos Santos,
Poliany Graziella de Freitas,
Juliana Barbosa Nunes,
Marcos José Marques,
Camila G.D. Padovani,
Wagner Alves de Souza Júdice,
Ihosvany Camps,
Nelson José Freitas da Silveira,
Diogo Teixeira Carvalho,
Márcia Paranho Veloso
Publication year - 2017
Publication title -
journal of the brazilian chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.337
H-Index - 70
eISSN - 1678-4790
pISSN - 0103-5053
DOI - 10.21577/0103-5053.20170192
Subject(s) - eugenol , chemistry , combinatorial chemistry , biochemical engineering , computational biology , organic chemistry , biology , engineering
The present study evaluated the inhibitory activity of new eugenol esters on Leishmania rCPB 2.8 enzyme aiming to discover new promising drug candidates. Activation and enhancement of the in vitro proteolytic activity of this enzyme were also produced by some compounds and may be related to their preference in binding to an allosteric site, possibly located in the region of the LYS159 residue, close to the active site. Details are presented in the Article Design, Synthesis, Biological Evaluation and Molecular Modeling Studies of Novel Eugenol Esters as Leishmanicidal Agents by Camila M. Coelho, Thiago dos Santos, Poliany G. Freitas, Juliana B. Nunes, Marcos J. Marques, Camila G. D. Padovani, Wagner A. S. Júdice, Ihosvany Camps, Nelson J. F. da Silveira, Diogo T. Carvalho and Marcia P. Veloso on page 715.
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