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1.
ChemistryOpen ; 10(10): 930, 2021 10.
Article in English | MEDLINE | ID: mdl-34596971

ABSTRACT

Invited for this month's cover picture is the group of Prof. Fernanda Andreia Rosa at the State University of Maringá (Brazil). The cover picture shows the contribution of the SINTHET research group to the synthesis and discovery of new antiprotozoal compounds. The synthetic methodology allowed the construction of 60 new isoxazole derivatives with structural variations on the 3-, 4-, and 5-positions. The authors acknowledge Ms. Jeniffer do Nascimento Ascencio Camargo and Ms. Julia Caroline Manzano Willig for the Cover picture creation. Read the full text of their Full Paper at 10.1002/open.202100141.

2.
ChemistryOpen ; 10(10): 931-938, 2021 10.
Article in English | MEDLINE | ID: mdl-34331350

ABSTRACT

A series of 60 4-aminomethyl 5-aryl-3-substituted isoxazoles were synthesized by an efficient method and evaluated in vitro against Leishmania amazonensis and Trypanosoma cruzi, protozoa that cause the neglected tropical diseases leishmaniasis and Chagas disease, respectively. Thirteen compounds exhibited a selective index greater than 10. The series of 3-N-acylhydrazone isoxazole derivatives bearing the bithiophene core exhibited the best antiparasitic effects.


Subject(s)
Antiprotozoal Agents , Leishmaniasis , Trypanosoma cruzi , Antiprotozoal Agents/pharmacology , Antiprotozoal Agents/therapeutic use , Humans , Isoxazoles/therapeutic use , Leishmaniasis/drug therapy , Structure-Activity Relationship
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