Journal
MOLECULES
Volume 21, Issue 11, Pages -Publisher
MDPI
DOI: 10.3390/molecules21111483
Keywords
Morita-Baylis-Hillman adducts; Leishmania amazonensis; eugenol; thymol; carvacrol
Funding
- CNPq
- CAPES
- PRPG-UFPB
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Leishmaniasis represents a series of severe neglected tropical diseases caused by protozoa of the genus Leishmania and is widely distributed around the world. Here, we present the syntheses of Morita-Baylis-Hillman adducts (MBHAs) prepared from eugenol, thymol and carvacrol, and their bioevaluation against promastigotes of Leishmania amazonensis. The new MBHAs are prepared in two steps from essential oils in moderate to good yields and present IC50 values in the range of 22.30-4.71 mu M. Moreover, the selectivity index to the most potent compound is very high (SIrb > 84.92), far better than that of Glucantime (R) (SIrb 1.39) and amphotericin B (SIrb = 22.34). Conformational analysis were carried out at the M062X//6-31+G(d,p) level of theory to corroborate a hypothesis about the nitroaromatic bioreduction mechanism.
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