1173709-57-3Relevant articles and documents
Alkyl and aryl derivatives based on p-coumaric acid modification and inhibitory action against leishmania braziliensis and plasmodium falciparum
De Sousa, Dami?o P.,Lopes, Susiany P.,Pérez-Castillo, Yunierkis,Robledo, Sara M.,Yepe, Lina M.
, (2020)
In low-income populations, neglected diseases are the principal cause of mortality. Of these, leishmaniasis and malaria, being parasitic, protozoan infections, affect millions of people worldwide and are creating a public health problem. The present work evaluates the leishmanicidal and antiplasmodial action of a series of twelve p-coumaric acid derivatives. Of the tested derivatives, eight presented antiparasitic activities 1-3, 8-12. The hexyl p-coumarate derivative (9) (4.14 ± 0.55 μg/mL; selectivity index (SI) = 2.72) showed the highest leishmanicidal potency against the Leishmania braziliensis amastigote form. The results of the molecular docking study suggest that this compound inhibits aldehyde dehydrogenase (ALDH), mitogen-activated kinase protein (MPK4), and DNA topoisomerase 2 (TOP2), all of which are key enzymes in the development of Leishmania braziliensis. The data indicate that these enzymes interact via Van derWaals bonds, hydrophobic interactions, and hydrogen bonds with phenolic and aliphatic parts of this same compound. Of the other compounds analyzed, methyl p-coumarate (64.59 ± 2.89 μg/mL; IS = 0.1) demonstrated bioactivity against Plasmodium falciparum. The study reveals that esters presenting a p-coumarate substructure are promising for use in synthesis of derivatives with good antiparasitic profiles.
P-coumarate as well as synthesis method and application thereof
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Paragraph 0057-0058, (2021/09/21)
The invention discloses p-coumarate as well as a synthesis method and application thereof. The method comprises the following steps: adding methyl p-coumarate, alcohols and a catalyst into a solvent, uniformly mixing to obtain a mixed solution, and heating in an oscillating state for reaction to obtain the p-coumarate. According to the transesterification method, enzymatic transesterification reaction is carried out in a non-aqueous phase system, the obvious defects of poor selectivity, high reagent toxicity, harsh conditions and the like of traditional chemical catalysis are overcome, the activity is maintained and enhanced, the conditions are mild, the selectivity is high, the operation is simple, the yield is relatively high, the reaction time is shortened, and the application prospect is good.
Synthesis and DNA polymerase α and β inhibitory activity of alkyl p-coumarates and related compounds
Nishimura, Katsumi,Takenaka, Yukiko,Kishi, Manami,Tanahashi, Takao,Yoshida, Hiromi,Okuda, Chiaki,Mizushina, Yoshiyuki
experimental part, p. 476 - 480 (2009/12/28)
trans- and cis-Icosyl, docosyl, and tetracosyl p-coumarates, constituents of Artemisia annua L., and their structurally-related compounds were synthesized and evaluated for inhibitory activity on DNA polymerases α and β. Among 30 compounds synthesized, oc
