The Bioactivity of Xylene, Pyridine, and Pyrazole Aza Macrocycles against Three Representative Species.

Pharmaceutics

Departamento de Parasitología, Instituto de Investigación Biosanitaria (IBS. Granada), Hospitales Universitarios de Granada, Universidad de Granada, Severo Ochoa s/n, 18071 Granada, Spain.

Published: March 2023

Due to the urgent need for finding effective and free of secondary effect treatments for every clinical form of Leishmaniasis, a series of synthetic xylene, pyridine and, pyrazole azamacrocycles were tested against three species. A total of 14 compounds were tested against J774.2 macrophage cells which were models for host cells, and against promastigote and amastigote forms of each studied parasite. Amongst these polyamines, one proved effective against another one for and and another one was selective solely for These compounds showed leishmanicidal activity and reduced parasite infectivity and dividing ability. Action mechanism studies gave a hint that compounds were active against due to their ability to alter parasite metabolic pathways and reduce (except Py33333) parasitic Fe-SOD activity.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10059905PMC
http://dx.doi.org/10.3390/pharmaceutics15030992DOI Listing

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