Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 33, Issue 1, Pages 210-226Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1410480
Keywords
Leishmania tropica and infantum; promastigotes; anti-leishmania agents; alkyl benzimidazolium salts; 2-benzyl-1-lupinylbenzimidazole derivatives
Funding
- Ministero dell'Istruzione, dell'Universita e della Ricerca (PRIN) [2010C2LKKJ_006, 20154JRJPP_004]
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Two sets of benzimidazole derivatives were synthesised and tested in vitro for activity against promastigotes of Leishmania tropica and L. infantum. Most of the tested compounds resulted active against both Leishmania species, with IC50 values in the low micromolar/sub-micromolar range. Among the set of 2-(long chain)alkyl benzimidazoles, whose heterocyclic head was quaternised, compound 8 resulted about 100-/200-fold more potent than miltefosine, even if the selectivity index (SI) versus HMEC-1 cells was only moderately improved. In the set of 2-benzyl and 2-phenyl benzimidazoles, bearing a basic side chain in position 1, compound 28 (2-(4-chlorobenzyl)-1-lupinyl-5-trifluoromethylbenzimidazole) was 12-/7-fold more potent than miltefosine, but exhibited a further improved SI. Therefore, compounds 8 and 28 represent interesting hit compounds, susceptible of structural modification to improve their safety profiles. [GRAPHICS] .
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