35354-29-1Relevant articles and documents
Polyhydroxybenzoic acid derivatives as potential new antimalarial agents
Degotte, Gilles,Francotte, Pierre,Pirotte, Bernard,Frédérich, Michel
, (2021/08/07)
With more than 200 million cases and 400,000 related deaths, malaria remains one of the deadliest infectious diseases of 2021. Unfortunately, despite the availability of efficient treatments, we have observed an increase in people infected with malaria since 2015 (from 211 million in 2015 to 229 million in 2019). This trend could partially be due to the development of resistance to all the current drugs. Therefore, there is an urgent need for new alternatives. We have, thus, selected common natural scaffolds, polyhydroxybenzoic acids, and synthesized a library of derivatives to better understand the structure–activity relationships explaining their antiplasmodial effect. Only gallic acid derivatives showed a noticeable potential for further developments. Indeed, they showed a selective inhibitory effect on Plasmodium (IC50 ~20 μM, SI > 5) often associated with interesting water solubility. Moreover, this has confirmed the critical importance of free phenolic functions (pyrogallol moiety) for the antimalarial effect. Methyl 4-benzoxy-3,5-dihydroxybenzoate (39) has, for the first time, been recognized as a potential lead for future research because of its marked inhibitory activity against Plasmodium falciparum and its significant hydrosolubility (3.72 mM).
Preparation method of 3,5-dihydroxybenzyl alcohol
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Paragraph 0007; 0011; 0012, (2017/05/27)
The invention relates to a preparation method of a medical and chemical intermediate 3,5-dihydroxybenzyl alcohol. The method comprises the following steps of: with commercially available 3,5-dihydroxy-benzoic acid as a raw material, preparing 3,5-diacetoxybenzoic acid through an acetylation reaction; reducing carboxyl into alcohol by a sodium borohydride/iodine borohydride system; and finally, performing acetyl de-protection using a weak base solution to obtain the target product 3,5-dihydroxybenzyl alcohol. The synthesis path has the characteristics of cheap and easily available reagent, mild reaction conditions, easiness in operation, easiness in product separation, relatively high yield and the like.
Bimolecular catalysis and turnover from a macromolecular host system
Ellis, Adam,Gooch, David,Twyman, Lance J
, p. 5364 - 5371 (2013/07/26)
The synthesis of a globular macromolecule and its application as a bimolecular catalyst are reported. The macromolecular structure supports (at least) two zinc-metalated porphyrin units, each capable of binding a single reactant. The proximity of the two