The Bioactivity of Xylene, Pyridine, and Pyrazole Aza Macrocycles against Three Representative <i>Leishmania</i> Species
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 <i>Leishmania</i> species. A total of 14 compounds were tested agai...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
| Published: |
MDPI AG,
2023-03-01T00:00:00Z.
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| Summary: | 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 <i>Leishmania</i> 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 <i>Leishmania</i> parasite. Amongst these polyamines, one proved effective against <i>L. donovani,</i> another one for <i>L. braziliensis</i> and <i>L. infantum,</i> and another one was selective solely for <i>L. infantum.</i> These compounds showed leishmanicidal activity and reduced parasite infectivity and dividing ability. Action mechanism studies gave a hint that compounds were active against <i>Leishmania</i> due to their ability to alter parasite metabolic pathways and reduce (except Py33333) parasitic Fe-SOD activity. |
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| Item Description: | 10.3390/pharmaceutics15030992 1999-4923 |