| Autor: |
Camargo, Jeniffer do Nascimento Ascencio, Pianoski, Karlos Eduardo, dos Santos, Mariellen Guilherme, Lazarin-Bidóia, Danielle, Volpato, Hélito, Moura, Sidnei, Nakamura, Celso Vataru, Rosa, Fernanda Andreia |
| Předmět: |
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| Zdroj: |
Frontiers in Pharmacology; 10/7/2020, Vol. 11, pN.PAG-N.PAG, 10p |
| Abstrakt: |
A series of trifluoromethylated pyrazole thiosemicarbazone, trifluromethylated pyrazole isothiosemicarbazone, and trifluoromethylated pyrazole 2-amino-1,3,4-thiadiazole hybrids were synthesized and evaluated in vitro against the promastigote form of Leishmania amazonensis and the epimastigote form of Trypanosoma cruzi , the pathogens causing the neglected tropical diseases leishmaniasis and Chagas disease, respectively. The results show the potential of these compounds regarding their antiparasitic properties. Studies on the structure-activity relationship demonstrated that compounds containing a bulky group at the para position of the phenyl ring attached to the 5-position of the pyrazole core had better antiparasitic effects. Among the substituents attached at the 3-position of the pyrazole ring, the insertion of the 2-amino-1,3,4-thiadiazole nucleus led to the most potent compounds compared to the thiosemicarbazone derivative. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
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