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We employed helical phasing analysis to study DNA conformation in the absence and presence of PUT3, a member of the Zn 2 Cys 6 binuclear cluster family of transcription factors. Our data indicate that the PUT3 target site UAS 10 does not bend appreciably in the absence of PUT3(1–100), but bends...
Phosphorothioates kill the procyclic form of T. brucei brucei by a non antisense but sequence dependent effect. The alamar Blue TM method allowed an easy microscale determination of their antiparasitic effect. The LD 50 of the sequences tested was in the range of 11–20 μM.
A practical and enantioselective total synthesis of the mercapturic acid sulfoxide 4 , a metabolite of anti-inflammatory drug DUP 697 1 , has been accomplished by employing the substratecontrolled diastereoselective oxidation of the sulfide 7 to the sulfoxide 8 as the key step. This led to the...
Photoactivatable benzophenone-containing analogs of isoprenyl diphosphates have been synthesized and evaluated as substrates and inhibitors of three bacterial prenyltransferases: farnesyl diphosphate synthase (FPS), hexaprenyl diphosphate synthase (HexPS) and undecaprenyl diphosphate synthase...
Five new 7-hydroxy-8-(N-alkylaminomethyl)coumarin labels ( 6a-e ) were prepared from 4-(4-carboxybutyl)-7-hydroxycoumarin ( 4 ) in 28–48% yield. Compared to 4-methylumbelliferone (4-MU, 1 ), the new fluorescent labels exhibited higher emission intensity over a broader pH range. Extinction...
Fatty acid binding proteins are a class of small 15 kDa proteins with a simple architecture that forms a large solvent sequestered cavity. In previous work, we demonstrated that reductive amination reactions could be performed in this cavity by covalent attachment of a pyridoxamine cofactor to...
With the aim of understanding the influence of redox potentials on the trypanocidal activity, a series of quinones were tested in vitro with trypomastigotes of Trypanosoma cruzi and their first cathodic potentials (Ep cl ) measured by cyclic voltammetry. All quinones with Ep cl > −0.72V were...
A novel series of N-(4-(4-Phenylbenzoylamino)butyl)-1,2,3,4-tetrahydro-2-naphthylamines with high affinity and selectivity for the dopamine D 3 receptor has been prepared. The 5-cyclopropylmethyloxy 3j , methanesulfonyloxy 3k and trifluoromethanesulfonyloxy 3l derivatives represent some of the...
Remarkably diastereoselective and regioselective reactions on an equimolar mixture of D-ribose, D-arabinose, D-xylose and D-lyxose are reported to give 5- O -functionalised D-ribofuranose derivatives.
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