1219-38-1Relevant articles and documents
Preparation method of benzoic acid high-carbon alcohol ester
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Paragraph 0099-0101, (2020/03/09)
The invention provides a preparation method of a benzoic acid higher alcohol ester. According to the preparation method, the benzoic acid higher alcohol ester is prepared by reaction of a benzoic acidcompound and a high carbon alcohol under the action of a sulfonic acid modified heterogeneous catalyst. The method has the beneficial effects that the production cost is low, the production process is safe, the post-treatment is simple, a large amount of industrial wastewater is avoided, and the method is more suitable for industrial production.
Gibbilimbol analogues as antiparasitic agents - Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum
Varela, Marina T.,Dias, Roberto Z.,Martins, Ligia F.,Ferreira, Daiane D.,Tempone, Andre G.,Ueno, Anderson K.,Lago, Jo?o Henrique G.,Fernandes, Jo?o Paulo S.
, p. 1180 - 1183 (2016/02/23)
The essential oils from leaves of Piper malacophyllum (Piperaceae) showed to be mainly composed by two alkenylphenol derivatives: gibbilimbols A and B. After isolation and structural characterization by NMR and MS data analysis, both compounds were evaluated against promastigote/amastigote forms of Leishmania (L.) infantum as well as trypomastigote/amastigote forms of Trypanosoma cruzi. The obtained results indicated that gibbilimbol B displayed potential against the tested parasites and low toxicity to mammalian cells, stimulating the preparation of several quite simple synthetic analogues in order to improve its activity and to explore the preliminary structure-activity relationships (SAR) data. Among the prepared derivatives, compound LINS03003 (n-octyl-4-hydroxybenzylamine) displayed the most potent IC50 values of 5.5 and 1.8 μM against amastigotes of T. cruzi and L. (L.) infantum, respectively, indicating higher activity than the natural prototype. In addition, this compound showed remarkable selectivity index (SI) towards the intracellular forms of Leishmania (SI = 13.1) and T. cruzi (SI = 4.3). Therefore, this work indicated that preparation of synthetic compounds structurally based in the bioactive natural products could be an interesting source of novel and selective compounds against these protozoan parasites.
Discovery of a Small Molecule PDI Inhibitor That Inhibits Reduction of HIV-1 Envelope Glycoprotein gp120
Khan, Maola M. G.,Simizu, Siro,Lai, Ngit Shin,Kawatani, Makoto,Shimizu, Takeshi,Osada, Hiroyuki
experimental part, p. 245 - 251 (2012/03/26)
Protein disulfide isomerase (PDI) is a promiscuous protein with multifunctional properties. PDI mediates proper protein folding by oxidation or isomerization and disrupts disulfide bonds by reduction. The entry of HIV-1 into cells is facilitated by the PDI-catalyzed reductive cleavage of disulfide bonds in gp120. PDI is regarded as a potential drug target because of its reduction activity. We screened a chemical library of natural products for PDI-specific inhibitors in a high-throughput fashion and identified the natural compound juniferdin as the most potent inhibitor of PDI. Derivatives of juniferdin were synthesized, with compound 13 showing inhibitory activities comparable to those of juniferdin but reduced cytotoxicity. Both juniferdin and compound 13 inhibited PDI reductase activity in a dose-dependent manner, with IC50 values of 156 and 167 nM, respectively. Our results also indicated that juniferdin and compound 13 exert their inhibitory activities specifically on PDI but do not significantly inhibit homologues of this protein family. Moreover, we found that both compounds can inhibit PDI-mediated reduction of HIV-1 envelope glycoprotein gp120.
