20025-59-6Relevant academic research and scientific papers
Discovery of Small-Molecule Inhibitors of the ATPase Activity of Human Papillomavirus E1 Helicase
Faucher, Anne-Marie,White, Peter W.,Brochu, Christian,Grand-Ma?tre, Chantal,Rancourt, Jean,Fazal, Gulrez
, p. 18 - 21 (2007/10/03)
The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus E1 helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. This screen led to the discovery of (biphenyl-4-sulfonyl)acetic acid 1, which inhibits the ATPase activity of HPV type 6 E1 helicase with a low micromolar IC50 value. A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series.
Sulfone derivatives, process for their production and use thereof
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, (2008/06/13)
A compound represented by the formula: 1wherein R is a cyclic hydrocarbon group, or the like; W is a bond, or the like; X is a divalent hydrocarbon group, or the like; Y and Z are each independently —N(R6)— or the like; ring A is a nitrogen-containing heterocyclic ring, or the like; R5 and R6 are independently hydrogen atom, a hydrocarbon group, or the like; Z′ is imidoyl group, or the like; a is 0, 1 or 2; and b is 0 or 1, or a salt thereof.
Fenbufen, a new anti inflammatory analgesic: synthesis and structure activity relationships of analogs
Child,Osterberg,Sloboda,Tomcufcik
, p. 466 - 476 (2007/10/05)
100 analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti inflammatory tests and the 2 phenyl 1,4 benzoquinone writhing and inflamed paw pressure analgesic tests. Only 3 retained the same full spectrum of activity as fenbufen: dl 4 (4 biphenylyl) 4 hydroxybutyric acid, dl 4 (4 biphenylyl) 1,4 butanediol, and 4 biphenylacetic acid. Fenbufen had the same spectrum of activity as aspirin, phenylbutazone, and indomethacin in the 5 tests. In addition, dose response derived potencies show fenbufen more potent than aspirin and at least as potent as phenylbutazone in all 5 tests. Two related compounds were generally similar.
