20959-02-8Relevant academic research and scientific papers
Chemical Compounds
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Page/Page column 17, (2008/12/07)
The invention is directed to novel azaindole and azaindazole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): where R1, R2, T1, T2 and T3 are defined below. These compounds are useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, in particular in the treatment and prevention of disorders mediated by IKK2 mechanisms including inflammatory and tissue repair disorders. Such disorders include rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease).
erythro- and threo-2-Hydroxynonyl substituted 2-phenyladenines and 2-phenyl-8-azaadenines: Ligands for A1 adenosine receptors and adenosine deaminase
Biagi, Giuliana,Giorgi, Irene,Livi, Oreste,Pacchini, Federica,Rum, Pietro,Scartoni, Valerio,Costa, Barbara,Mazzoni, Maria Rosa,Giusti, Laura
, p. 221 - 233 (2007/10/03)
erythro-2-Phenyl-9-(2-hydroxy-3-nonyl)adenine and its 8-aza analog were prepared and showed a very high inhibitory activity towards adenosine deaminase (ADA), with Ki 0.55 and 1.67 nM, respectively, and high affinity for A1 adenosine receptors, with Ki 28 and 2.8 nM, respectively. To increase affinity for A1 receptors we introduced a substituent on the N6 position such as alkyl or cycloalkyl groups, which are present in effective agonists or antagonists. Furthermore, for some compounds, we prepared the two diastereoisomers erythro and threo to verify whether the binding with A1 receptors is stereoselective, as in ADA. Results show that some of the synthesised compounds are good inhibitors for ADA and good ligands for A1, and the erythro diastereoisomers are more active than the threo ones. The experimental evidence allows us to hypothesise some similarity in the three dimensional structures of the binding site of the two proteins, ADA and A1 adenosine receptor, in spite of lacking any homologies in the aminoacid sequences.
2-aryl-4,6-dihalopyrimidines as antidote for protecting cultivated plants from phytotoxic damage caused by herbicides
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, (2008/06/13)
2-Aryl-4,6-dihalopyrimidines of the formula I STR1 wherein Hal is halogen, E is unsubstituted or substituted phenyl, thienyl or furyl, and Y is a group bound by way of nitrogen, oxygen or sulfur, are able as antidote or `safener` to protect cultivated plants against the phytotoxic action of herbicides. Cultivated plants concerned are particularly sorghum, cereals, maize, rice and soya bean, and herbicides concerned are chloroacetanilides or other herbicidally effective substances.
