- Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies
-
Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
- Whittamore, Paul R.O.,Addie, Matthew S.,Bennett, Stuart N.L.,Birch, Alan M.,Butters, Michael,Godfrey, Linda,Kenny, Peter W.,Morley, Andrew D.,Murray, Paul M.,Oikonomakos, Nikos G.,Otterbein, Ludovic R.,Pannifer, Andrew D.,Parker, Jeremy S.,Readman, Kristy,Siedlecki, Pawel S.,Schofield, Paul,Stocker, Andy,Taylor, Melvyn J.,Townsend, Linda A.,Whalley, David P.,Whitehouse, Jennifer
-
p. 5567 - 5571
(2007/10/03)
-
- PROCESS AND INTERMEDIATES FOR THE PREPARATION OF THIENOPYRROLE DERIVATIVES
-
Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is a nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed.
- -
-
-
- Herbicidal Thienylureas, I
-
Syntheses of the title substances as potential herbicides are described by a modified Curtius degradation of corresponding thiophene carboxylic acids, obtained in turn by haloform reaction of appropriate acetyl thiophenes.Regioselective substitution reactions of thiophenes were key steps for the construction of desired substitution patterns.Structure-activity considerations show that especially the 3-thienyl ureas 36 and 38 exhibit significant herbicidal activity comparable with commercial products. - Keywords: Curtius degradation; Herbicides; Thiophenes; Ureas; Urethanes
- Stanetty, Peter,Puschautz, Erhard,Friedbacher, Gernot
-
-