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In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole‐Containing Azine and Benzoazine Derivatives
Author(s) -
MartínMontes Álvaro,
Kolodová Kristina,
Marín Clotilde,
RosalesLombardo María José,
SánchezMoreno Manuel,
AndrésGordo Lucía,
Cano Carmen,
Campayo Lucrecia,
GómezMuñoz Alberto,
Sanz Ana M.,
Yunta María J. R.
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100413
Subject(s) - trypanosoma cruzi , leishmania infantum , leishmania , leishmaniasis , imidazole , antiparasitic , leishmania donovani , chagas disease , antiparasitic agent , azine , stereochemistry , chemistry , benznidazole , antiprotozoal , leishmania braziliensis , biology , in vitro , visceral leishmaniasis , biochemistry , combinatorial chemistry , pharmacology , cutaneous leishmaniasis , virology , parasite hosting , medicine , organic chemistry , immunology , world wide web , computer science , pathology
Leishmaniasis and Chagas diseases are two of the most important parasitic diseases in the world. Both belong to the category of Neglected Tropical Diseases, and they cannot be prevented by vaccination. Their treatments are founded in outdated drugs that possess many pernicious side‐effects and they're not easy to administer. With the aim of discovering new compounds that could serve as anti‐trypanosomal drugs, an antiparasitic study of a synthetic compound family has been conducted. A series of new 1,4‐bis(alkylamino)‐ and 1‐alkylamino‐4‐chloroazine and benzoazine derivatives 1 – 4 containing imidazole rings have been synthesized and identified. Their structures showed a possible interest based on previous work. Their in vitro anti‐ Leishmania infantum , anti‐ L. braziliensis , anti‐ L. donovani and anti‐ T. cruzi activity were tested, as well as the inhibition of Fe‐SOD enzymes. It was found that some of them exhibited quite relevant values indicative of being worthy of future more detailed studies, as most of them showed activity to more than only one parasite species, especially compound 3 c was active for the three studied Leishmania species and also for T. cruzi , which is a very interesting trait as it covers a wide spectrum.