- Stereoselective fluorescence quenching in the electron transfer photooxidation of nucleobase-related azetidines by cyanoaromatics
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Electron transfer involving nucleic acids and their derivatives is an important field in bioorganic chemistry, specifically in connection with its role in the photo-driven DNA damage and repair. Four-membered ring heterocyclic oxetanes and azetidines have been claimed to be the intermediates involved in the repair of DNA (6-4) photoproduct by photolyase. In this context, we examine here the redox properties of the two azetidine isomers obtained from photocycloaddition between 6-aza-1,3-dimethyluracil and cyclohexene. Steady-state and time-resolved fluorescence experiments using a series of photoreductants and photooxidants have been run to evaluate the efficiency of the electron transfer process. Analysis of the obtained quenching kinetics shows that the azetidine compounds can act as electron donors. Additionally, it appears that the cis isomer is more easily oxidized than its trans counterpart. This result is in agreement with electrochemical studies performed on both azetidine derivatives.
- Fraga-Timiraos, Ana B.,Rodríguez-Mu?iz, Gemma M.,Peiro-Penalba, Vicente,Miranda, Miguel A.,Lhiaubet-Vallet, Virginie
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- Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors
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The invention concerns novel cyclohexane derivatives difunctionalised in 1.4 of general formula (1) in which A represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl or pyrimidinyl optionally substituted by one
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- 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT1A ligands
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A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I STR1 in which: R1 and R2, which are identical or different, represent hydrogen or C1 -C6 alkyl, n is 2 to 6, inclusive, A represents aryl piperazino II STR2 the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C1 -C3 alkyl, C1 -C3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino STR3 in which R represents hydrogen or C1 -C3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT1A receptor agonist therewith.
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