1514-26-7Relevant articles and documents
Evaluation of fluorinated biphenyl ether pro-drug scaffolds employing the chemical-microbial approach
Hampton, Alex S.,Mikulski, Lena,Palmer-Brown, William,Murphy, Cormac D.,Sandford, Graham
, p. 2255 - 2258 (2016)
Incorporation of fluorine in a drug can dramatically affect its metabolism and methods to assess the effect of fluorine substitution on drug metabolism are required for effective drug design. Employing a previously developed chemical-microbial method the metabolism of a series of fluorinated biphenyl ethers was determined. The substrates were synthesized via Ullmann-type condensation reactions between bromotoluene and fluorophenol. The ethers were incubated with the fungus Cunninghamella elegans, which oxidises xenobiotics in an analogous fashion to mammals, generating a number of hydroxylated biphenyl ethers and acids. The propensity of the fluorinated ring to be hydroxylated depended upon the position of the fluorine atom, and the oxidation of the methyl group was observed when it was meta to the oxygen. The experiments demonstrate the applicability of the method to rapidly determine the effect of fluorine substitution on CYP-catalysed biotransformation of pro-drug molecules.
N-[1-(3-phenoxyphenyl)ethyl]acetohydroxamic acid compounds which are useful anti-inflammatory agents
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, (2008/06/13)
The present invention provides compounds of formula (II) STR1 wherein q is 1, and p is 1; Ar is phenyl optionally substituted by one or more substitutents independently selected from C1-4 alkyl (which may be substituted by one or more halogen a
Anti-inflammatory aryl derivatives
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, (2008/06/13)
The present inventions concerned with compounds of formula (I) wherein, Ar is 4-halophenyl;, Ar? is 1,3- or 1,4-phenylene;, Y is (E)-CH=CH-; and, R1 and R2 are independently selected from hydrogen and C1-4alkyl;, and base salts and physiologica