In vitro Leishmanicidal and Trypanosomicidal Properties of Imidazole-Containing Azine and Benzoazine Derivatives.

Autor: Martín-Montes Á; Departamento de Parasitología, Facultad de Ciencias, Universidad de Granada, 18071, Granada, Spain., Kolodová K; Klinik und Poliklinik für Innere Medizin III, Universitätsklinikum Regensburg, Franz-Josef-Strauss-Allee 11, 93053, Regensburg, Germany., Marín C; Departamento de Parasitología, Facultad de Ciencias, Universidad de Granada, 18071, Granada, Spain., Rosales-Lombardo MJ; Departamento de Parasitología, Facultad de Ciencias, Universidad de Granada, 18071, Granada, Spain., Sánchez-Moreno M; Departamento de Parasitología, Facultad de Ciencias, Universidad de Granada, 18071, Granada, Spain., de Andrés-Gordo L; Centro Nacional de Investigaciones Oncológicas (CNIO), 28029, Madrid, Spain., Cano C; Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040, Madrid, Spain., Campayo L; Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040, Madrid, Spain., Gómez-Muñoz A; IES Jose Luis López Aranguren, 28945, Fuenlabrada, Madrid, Spain., Sanz AM; Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040, Madrid, Spain., Yunta MJR; Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040, Madrid, Spain.
Jazyk: angličtina
Zdroj: ChemMedChem [ChemMedChem] 2021 Dec 06; Vol. 16 (23), pp. 3600-3614. Date of Electronic Publication: 2021 Oct 19.
DOI: 10.1002/cmdc.202100413
Abstrakt: 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 Their treatments are founded in outdated drugs that possess many pernicious side-effects and they're not easy to administer.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.
(© 2021 The Authors. ChemMedChem published by Wiley-VCH GmbH.)
Databáze: MEDLINE
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