Antiparasitic Behavior of Trifluoromethylated Pyrazole 2-Amino-1,3,4-thiadiazole Hybrids and Their Analogues: Synthesis and Structure-Activity Relationship

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 o...

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Published inFrontiers in pharmacology Vol. 11; p. 591570
Main Authors 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
Format Journal Article
LanguageEnglish
Published Frontiers Media S.A 07.10.2020
Subjects
antileishmanial
antitrypanosomal
Pharmacology
thiadiazole
thiosemicarbazone
trifluoromethylated pyrazoles
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Summary: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.
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Reviewed by: Stevan Pecic, California State University, United States; Marcus Scotti, Federal University of Paraíba, Brazil
This article was submitted to Translational Pharmacology, a section of the journal Frontiers in Pharmacology
Edited by: Marta Carrasco, University of Lisbon, Portugal
ISSN:1663-9812
1663-9812
DOI:10.3389/fphar.2020.591570