Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes

In the present study a series of 34 synthetic ligustrazine-containing α, β-Unsaturated carbonyl-based compounds and oximes, recognized as anticancer compounds were assessed against protozoa of the Trypanosoma and Leishmania species. Ligustrazine, chemically known as tetramethylpyrazine (TMP), was se...

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Main Authors: Abdulsalam A. M. Alkhaldi, Harry P. de Koning, Syed Nasir Abbas Bukhari
Format: Article
Language:English
Published: Universidade de São Paulo 2021-10-01
Series:Brazilian Journal of Pharmaceutical Sciences
Subjects:
Online Access:http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502021000100524&tlng=en
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author Abdulsalam A. M. Alkhaldi
Harry P. de Koning
Syed Nasir Abbas Bukhari
author_facet Abdulsalam A. M. Alkhaldi
Harry P. de Koning
Syed Nasir Abbas Bukhari
author_sort Abdulsalam A. M. Alkhaldi
collection DOAJ
description In the present study a series of 34 synthetic ligustrazine-containing α, β-Unsaturated carbonyl-based compounds and oximes, recognized as anticancer compounds were assessed against protozoa of the Trypanosoma and Leishmania species. Ligustrazine, chemically known as tetramethylpyrazine (TMP), was selected as the core moiety for the synthesis of α, β-Unsaturated carbonyl-based compounds and these compounds were selected as precursors for the synthesis of new oximes. Some derivates, including 5f and 6i, showed multiple activities against all tested strains. In particular compounds 5f and 8o are the most potent and they are, therefore, potential candidates for trypanosomiasis and leishmaniasis
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spelling doaj.art-23d9b47c8cfb4830b7306357825ccc132022-12-21T23:28:29ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-97902021-10-015710.1590/s2175-97902020000418997Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentesAbdulsalam A. M. AlkhaldiHarry P. de KoningSyed Nasir Abbas Bukharihttps://orcid.org/0000-0001-8125-7972In the present study a series of 34 synthetic ligustrazine-containing α, β-Unsaturated carbonyl-based compounds and oximes, recognized as anticancer compounds were assessed against protozoa of the Trypanosoma and Leishmania species. Ligustrazine, chemically known as tetramethylpyrazine (TMP), was selected as the core moiety for the synthesis of α, β-Unsaturated carbonyl-based compounds and these compounds were selected as precursors for the synthesis of new oximes. Some derivates, including 5f and 6i, showed multiple activities against all tested strains. In particular compounds 5f and 8o are the most potent and they are, therefore, potential candidates for trypanosomiasis and leishmaniasishttp://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502021000100524&tlng=enProtozoan parasites. Sleeping sickness. α,β-Unsaturated carbonyl-based compoundstoxicity. Organic synthesis
spellingShingle Abdulsalam A. M. Alkhaldi
Harry P. de Koning
Syed Nasir Abbas Bukhari
Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
Brazilian Journal of Pharmaceutical Sciences
Protozoan parasites. Sleeping sickness. α,β-Unsaturated carbonyl-based compounds
toxicity. Organic synthesis
title Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
title_full Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
title_fullStr Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
title_full_unstemmed Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
title_short Synthetic ligustrazine based cyclohexanone and oxime analogs as Anti-Trypanosoma and Anti-Leishmanial agentes
title_sort synthetic ligustrazine based cyclohexanone and oxime analogs as anti trypanosoma and anti leishmanial agentes
topic Protozoan parasites. Sleeping sickness. α,β-Unsaturated carbonyl-based compounds
toxicity. Organic synthesis
url http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502021000100524&tlng=en
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