English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Plus monthly

Global: Zendy Tools annual

Global: Zendy Tools monthly

Global: Zendy Free Plan

There is an urgent need for better drugs for a more successful fight against leishmaniasis, one of the most important neglected diseases caused by the parasite Leishmania. We have recently synthesized several symmetrical pyridinium compounds belonging to two dif‐ ferent series: bis-pyridinium and bis-quinolinium acyclic structures and bis-pyridinium diazacyclophanes derivatives. The first series of bis-pyridinium derivatives have been found to display activity against promastigotes and intracellular amastigotes of Leishma‐ nia donovani and Leishmania major, with EC50 values lower than 1 μM. The majority of compounds show a similar behavior in both Leishmania species, being slightly more active against intracellular amastigotes of L. major. The series of bis-pyridinium diazacyclo‐ phanes can be considered as rigid analogues of the previous bis-cationic ones. The activi‐ ty of these compounds has also been evaluated against promastigotes and intracellular amastigotes of L. donovani and L. major. All the diazacyclophanes are more active against L. major, with EC50 values of between 1 and 17 μM in intracellular amastigotes, and in some cases they present a higher selectivity index than the reference anti-leishmanial drugs such as amphotericin B and miltefosine. In conclusion, these bis-quaternary com‐ pounds represent promising candidates as potential therapeutic agents against leishma‐ niasis.

Symmetrical Pyridinium-Phanes and –Diazacyclophanes — Promising Heterocyclic Scaffolds for the Development of Anti-Leishmanial Agents