AUTHOR=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 

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

JOURNAL=Frontiers in Pharmacology

VOLUME=11

YEAR=2020

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2020.591570

DOI=10.3389/fphar.2020.591570

ISSN=1663-9812

ABSTRACT=<p>A series of trifluoromethylated pyrazole thiosemicarbazone, trifluromethylated pyrazole isothiosemicarbazone, and trifluoromethylated pyrazole 2-amino-1,3,4-thiadiazole hybrids were synthesized and evaluated <italic>in vitro</italic> against the promastigote form of <italic>Leishmania amazonensis</italic> and the epimastigote form of <italic>Trypanosoma cruzi</italic>, 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 <italic>para</italic> 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.</p>