352017-39-1Relevant academic research and scientific papers
Aza analogues of thalidomidesynthesis and evaluation as inhibitors of tumor necrosisfactor-α production in vitro
Gütschow, Michael,Hecker, Thomas,Thiele, Andrea,Hauschildt, Sunna,Eger, Kurt
, p. 1059 - 1065 (2001)
A synthetic entry to derivatives of the new classes of 5-phthalimidouracils and 5-phthalimidobarbituric acids is reported. These 5-phthalimidopyramines as well as phthalimido-2,4-difluorobenzenes were designed as analogues of thalidomide, a well known inhibitor of TNF-α production. A preliminary in vitro investigation of the compounds as inhibitors of the TNF-α production was performed. Among the compounds of the present series, (5-ethyl-1-phenyl-5- tetrafluorophthalimido)barbituric acid and (2- 2,4-difluorophenyl)-4,5,6,7-tetrafluoro-1H-isoindole-1,3 2H)-dione were proved to be potent inhibitors. Both compounds showed inhibitory activity in the lower micromolar range of the LPS-induced TNF-α production in human monocytes. Copyright
