Synthesis and biological evaluation of 3-substituted-benzofuran-2- carboxylic esters as a novel class of ischemic cell death inhibitors
A series of 3-substituted-benzofuran-2-carboxylic esters was synthesized and evaluated for biological activity as ischemic cell death inhibitors in H9c2 cells and rat primary cardiac myocytes under conditions of oxygen and glucose deprivation. The introduction of a sulfur atom at the three-position substituent of the benzofuran ring markedly improved ischemic cell death inhibitory potency. In particular, 3-[2-(4-nitro-phenylsulfanyl)-acetylamino]-benzofuran-2- carboxylic acid ester (10) (EC50 = 0.532 μM, cell death = 6.18%) and 4-chloro-3-[3-(pyridin-2-ylsulfanyl)-propionylamino]-benzofuran-2-carboxylic ester (18) (EC50 = 0.557 μM, cell death = 7.02%) were shown to be the most potent in this series of benzofuran analogs.
BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES SUBSTITUTED WITH AMIDE, PROCESS FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
The present invention relates to a novel benzofuran or benzothiophene derivative substituted with amide. The inventive benzofuran or benzothiophene derivative substituted with amide effectively inhibits ischemic cell death, and thus, can be advantageously
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(2009/05/28)
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