Peter Ventura, Alejandra M. published the artcileSynthesis and antischistosomal activity of linker- and thiophene-modified biaryl alkyl carboxylic acid derivatives, Recommanded Product: 3-(Methoxycarbonyl)benzoic acid, the publication is Archiv der Pharmazie (Weinheim, Germany) (2021), 354(12), 2100259, database is CAplus and MEDLINE.
Schistosomiasis is a neglected tropical disease caused by blood flukes of the genus Schistosoma and causes severe morbidity in infected patients. In 2018, 290.8 million people required treatment, and 200,000 deaths are reported per yr. Treatment of this disease depends on a single drug, praziquantel (PZQ). However, in the past few years, reduced sensitivity of the parasites toward PZQ has been reported. Therefore, there is an urgent need for new drugs against this disease. In the past few years, we have focused on a new substance class called biaryl alkyl carboxylic acid derivatives, which showed promising antischistosomal activity in vitro. Structure-activity relationship (SAR) studies of the carboxylic acid moiety led to three promising carboxylic amides (morpholine, thiomorpholine, and Me sulfonyl piperazine) with an antischistosomal activity down to 10μM (morpholine derivative) and no cytotoxicity up to 100μM. Here, we show our continued work on this substance class. We investigated, in extended SAR studies, whether modification of the linker and the thiophene ring could improve the antischistosomal activity. We found that the exchange of the alkyl linker by a pentadienyl or benzyl linker was tolerated and led to similar antischistosomal effects, whereas the exchange of the thiophene ring was not tolerated. Our data suggest that the thiophene ring is important for the antischistosomal activity of this compound class.
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, Recommanded Product: 3-(Methoxycarbonyl)benzoic acid.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics