Alves Avelar, Leandro A. published the artcileDesign and Synthesis of Novel Anti-Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit, Quality Control of 1877-71-0, the publication is Archiv der Pharmazie (Weinheim, Germany) (2017), 350(3-4), n/a, database is CAplus and MEDLINE.
Despite recent declines in mortality, malaria remains an important global health problem. New therapies are needed, including new drugs with novel modes of action compared to existing agents. Among new potential therapeutic targets for malaria, inhibition of parasitic histone deacetylases (HDACs) is a promising approach. Homol. modeling of PfHDAC1, a known target of some anti-plasmodial HDAC inhibitors, revealed a unique threonine residue at the rim of the active site in close proximity to the location of the cap group of vorinostat-type HDAC inhibitors. Aiming to obtain HDAC inhibitors with potent and preferential anti-plasmodial activity, the authors synthesized a mini-library of alkoxyamide-based HDAC inhibitors containing hydrogen bond acceptors in the cap group. Using a 5-step synthetic route, 12 new inhibitors were synthesized and assayed against Plasmodium falciparum asexual blood stage parasites (clones 3D7 and Dd2) and human cells (HepG2). The most active compound 6h (6-[(1-Benzothiophen-2-ylformamido)oxy]-N-hydroxyhexanamide) (Pf3D7 IC50: 0.07 μM; PfDd2 IC50: 0.07 μM) was 25-fold more toxic against the parasite vs. human HepG2 cells. Selected compounds were shown to cause hyperacetylation of P. falciparum histone H4, indicating inhibition of one or more PfHDACs.
Archiv der Pharmazie (Weinheim, Germany) published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Quality Control of 1877-71-0.
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https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics