113162-36-0Relevant articles and documents
Synthesis and structure of fluoroindole nucleosides
Bozilovic, Jelena,Bats, Jan W.,Engels, Joachim W.
, p. 283 - 292 (2008/02/11)
Chemically modified bases are frequently used to stabilize nucleic acids, to study the driving forces for nucleic acid structure formation, and to tune DNA and RNA hybridization conditions. Nucleoside analogues are chemical means to investigate hydrogen bonds, base stacking, and solvation as the three predominant forces that are responsible for the stability of nucleic acids. To obtain deeper insight into the contributions of these interactions to RNA stability, we decided to synthesize some novel nucleic acid analogues where the nucleobases are replaced by fluoroindoles. Fluorinated indoles can be compared with fluorinated benzimidazoles to determine the role of nitrogen in five-membered ring systems. The synthesis of fluoroindole ribonucleosides as well as the X-ray crystal structures of all synthesized fluoroindole ribonucleosides are reported here. These compounds could also be building blocks for a variety of biologically active RNA analogues.
Tripeptidyl peptidase inhibitors
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Page column 20, (2010/11/29)
The invention is relative to a compound of formula (I) and its use as an inhibitor of the CCK-inactivating peptidase tripeptidyl peptidase (TPP II). The invention concerns in particular the treatment of eating disorder, obesity, psychotic syndrome and associated psychiatric disorders. It concerns also the cosmetic use of a compound (I) in particular to aid slimming.
Indoline Analogues of Idazoxan: Potent α2-Antagonists and α1-Agonists
Fagan, Gay P.,Chapleo, Christopher B.,Lane, Anthony C.,Myers, Malcolm,Roach, Alan G.,et al
, p. 944 - 948 (2007/10/02)
The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described.Substitution in the indoline ring generated compounds with a spectrum of adrenoceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent.Many of the derivatives possess greater presynaptic antagonist potency that the corresponding benzodioxan 1, dihydrobenzofuran 2, and indan 3 analogues; however, this α2-antagonism is often accompanied by α1-agonist activity.It was not possible to separate α2-antagonist from α1-agonist properties in this series.Compounds of most interest proved to be the N-ethyl 6, 5-chloro-N-methyl 18 and 5-chloro-N-ethyl 23 derivatives, all being potent α2-antagonists and α1-agonists.Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties.