- 4-Heterosubstituted Cyclopentenone Antiviral Compounds: Synthesis, Mechanism, and Antiviral Evaluation
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Racemic 4-oxocyclopent-2-en-1-yl acetate was used in a short synthesis of nucleoside analogues with pyrimidine and purine heterobases. The protocol is based on a typical nucleophilic substitution process. Uracil, thymine, 6-chloropurine, and some adenines gave the expected 4-heterosubstituted products along with the isomeric 2-heterosubstituted compounds as minor components. Samples of selected products were evaluated for their antiviral activity in a primary screening against a variety of viruses belonging to different classes. One of the compounds was found to be highly active against human papilloma virus (HPV).
- Mantione, Daniele,Aizpuru, Olatz Olaizola,Memeo, Misal Giuseppe,Bovio, Bruna,Quadrelli, Paolo
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p. 983 - 991
(2016/03/01)
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- 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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- Synthesis and antiviral evaluation of bis(POM) prodrugs of (E)-[4′-phosphono-but-2′-en-1′-yl]purine nucleosides
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Seventeen hitherto unknown bis(POM) prodrugs of novel (E)-[4′- phosphono-but-2′-en-1′-yl]purine nucleosides were prepared in a straight approach and at good yields. Those compounds were synthesized by the reaction of purine nucleobases directly with the p
- Pradère, Ugo,Roy, Vincent,Montagu, Aurélien,Sari, Ozkan,Hamada, Manabu,Balzarini, Jan,Snoeck, Robert,Andrei, Graciela,Agrofoglio, Luigi A.
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p. 126 - 133
(2013/01/15)
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- Microwave-assisted regioselective synthesis of acyclic nucleosides through an alkylating reaction with 2-oxa-1,4-butanediol diacetate
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An efficient and green procedure for the synthesis of purine acyclic nucleosides through microwave-assisted, alkylation of various purine nucleobases with 2-oxa-1,4-butanediol diacetate in the absence of solvent and catalyst is described. The advantages of using this method include its environmental friendliness, simple manipulation, short reaction time, high regioselectivity, and good yields.
- Qu, Guirong,Han, Suhui,Zhang, Zhiguang,Geng, Mingwei,Xue, Feng
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p. 819 - 824
(2007/10/03)
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