Clemente, Camila M. published the artcileEugenol carbonate activity against Plasmodium falciparum, Leishmania braziliensis, and Trypanosoma cruzi, Quality Control of 111-87-5, the main research area is allyl methoxyphenyl alkylcarbonate preparation antiparasitic activity; antiplasmodial activity; leishmanicidal activity; molecular docking; trypanocidal activity.
Neglected tropical diseases are a major health problem throughout the world, and there are few effective and safe drugs. In this study, we report the design and synthesis of a novel series of carbonates of eugenol using different aliphatic alcs. and N,N-carbonyldiimidazole. Spectroscopic techniques, including 1H NMR (NMR), 13C NMR, Fourier transform IR, and high-resolution mass spectrometry, were used to confirm the structures of the synthesized compounds In vitro and in silico studies of prodrugs of eugenol were performed to determine their antiplasmodial, trypanocidal, and leishmanicidal activities, and also their cytotoxicity. Compounds were highly active against Leishmania braziliensis and Plasmodium falciparum, whereas the activity shown for Trypanosoma cruzi was moderate. Mol. docking was used to determine a possible mode of action of eugenol against the dihydroorotate dehydrogenase of the three parasites (TcDHODH, LbDHODH, and PfDHODH). Notably, the docking results showed that eugenol not only has binding energy similar to that of the natural substrate (-7.2 and -7.1, resp.) but also has interactions with relevant biol. residues of PfDHODH. This result indicates that eugenol could act as a substrate for PfDHODH in the pyrimidine biosynthesis pathway of P. falciparum. In conclusion, the combination of certain aliphatic alcs. and eugenol through a carbonate bond could significantly increase the antiparasitic activity of this class of compounds, which merits further studies.
Archiv der Pharmazie (Weinheim, Germany) published new progress about Antimalarials. 111-87-5 belongs to class alcohols-buliding-blocks, name is n-Octanol, and the molecular formula is C8H18O, Quality Control of 111-87-5.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts