Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.

@article{Oinuma1991SynthesisAB,
  title={Synthesis and biological evaluation of substituted benzenesulfonamides as novel potent membrane-bound phospholipase A2 inhibitors.},
  author={Hitoshi Oinuma and Tadanobu Takamura and Takuro Hasegawa and Ken ‘ ichi Nomoto and Tomomichi Naitoh and Y Daiku and Shuichi Hamano and H Kakisawa and Narihiro Minami},
  journal={Journal of medicinal chemistry},
  year={1991},
  volume={34 7},
  pages={2260-7}
}
A novel series of 4-[N-methyl-N-[(E)-3-[4-(methylsulfonyl)phenyl]-2- propenoyl]amino]benzenesulfonamides has been prepared and evaluated as membrane-bound phospholipase A2 inhibitors. A structure-activity relationship study indicated that the optimum potency was realized with the N-(phenylalkyl)piperidine derivatives 3 and 4. These compounds inhibited the liberation of arachidonic acid from the rabbit heart membrane fraction with IC30 values of 0.028 and 0.009 microM, respectively. Several… CONTINUE READING