Peter Ventura, Alejandra M.; Haeberlein, Simone; Konopka, Leonie; Obermann, Wiebke; Gruenweller, Arnold; Grevelding, Christoph G.; Schlitzer, Martin published their research in Archiv der Pharmazie (Weinheim, Germany) on December 31 ,2021. The article was titled 《Synthesis and antischistosomal activity of linker- and thiophene-modified biaryl alkyl carboxylic acid derivatives》.Related Products of 1877-71-0 The article contains the following contents:
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. The results came from multiple reactions, including the reaction of 3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0Related Products of 1877-71-0)
3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Related Products of 1877-71-0 Polyesters are important plastics, with monomers linked by ester moieties.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics