294673-72-6Relevant articles and documents
Synthesis and structure-activity relationship studies of conformationally restricted, analogs of 2-chloro-4-trifluoromethylpyrimidine- 5-[N-(3',5'-bis(trifluoromethyl)phenyl)]carboxamide
Palanki, Moorthy S.S.,Erdman, Paul E.,Goldman, Mark E.,Suto, Carla,Suto, Mark J.
, p. 19 - 29 (2007/10/03)
2-Chloro-4-trifluoromethylpyrimidine-5-N[(3,5- bis(trifluoromethyl)phenyl] carboxamide (1) was identified as an inhibitor of AP-1 and NF-κB mediated transcriptional activation. In an effort to identify novel compounds that contain less number of trifluoromethyl groups with comparable potency as 1, several conformationally restricted analogs of I were synthesized in which the pyrimidine ring and the aniline ring were connected through a second 'bridge'. The 7-membered sulfur bridged analog was the most potent in this series, and comparable to 1 in activity.