- Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
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The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
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Paragraph 0051-0052
(2014/10/16)
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- Convenient and efficient syntheses of N6-and N 4-substituted adenines and cytosines and their 2-deoxyribosides
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Convenient and efficient methods of the synthesis of N6-and N4-substituted derivatives of adenine and cytosine and their 2-deoxyribosides were developed. The reactions of either unprotected nucleobases (adenine, cytosine) or unprotected 2-deoxyribosides with aryl or alkyl aldehydes give corresponding Schiff bases that can be reduced to the target title compounds with high overall yields. In the case of aryl aldehydes the imine derivatives are obtained in the presence of methoxides in methanol and reduced with sodium borohydride. The corresponding reactions with alkyl aldehydes require the use of acetic acid and borane dimethyl sulfide complex instead.
- Adamska, Ewelina,Barciszewski, Jan,Markiewicz, Wojciech T.
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p. 861 - 871
(2013/02/23)
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- Lignopurines: A new family of hybrids between cyclolignans and purines. Synthesis and biological evaluation
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A new family of hybrids between cyclolignans related to podophyllic aldehyde, a non-lactonic cyclolignan, and purines were prepared and evaluated against several human tumour cell lines. Both fragments, cyclolignan and purine, were linked through aliphatic and aromatic chains. The influence on the cytotoxicity of the purine substitution and the nature of the linker is analyzed. The new family was slightly less cytotoxic than the parent podophyllic aldehyde, although the selectivity is maintained or even improved and among the linkers used, the presence of an aromatic ring gave the most potent and selective derivatives within the new series tested. Cell cycle and confocal studies demonstrate that these derivatives interfere with the tubulin polymerization and arrest cells at the G2/M phase, in the same way than the parent compounds podophyllotoxin and podophyllic aldehyde do.
- ángeles Castro,Miguel Del Corral, José M.,García, Pablo A.,Victoria Rojo,Bento, Ana C.,Mollinedo, Faustino,Francesch, Andrés M.,San Feliciano, Arturo
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supporting information
p. 377 - 389
(2013/02/23)
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- Process for preparing N6,9-disubstituted adenine
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A process for preparing N6, 9-disubstituted adenines which comprises reacting a metal salt of N6 -substituted adenine with a benzyl halide compound, preferably in the presence of a phase transfer catalyst. According to the process, the N6,9-disubstuted adenines can be obtained in high yields and good selectivity.
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