1018001-53-0Relevant articles and documents
Synthesis of pyrazolo[3,4-d]-4,5-dihydropyrimidin-6-ones
Ryabukhin, Sergey V.,Granat, Dmitry S.,Plaskon, Andrey S.,Shivanyuk, Alexander,Lukin, Oleg
, p. 1846 - 1847 (2014)
A small library of hitherto unprepared pyrazolo[3,4-d]-4,5- dihydropyrimidin-6-ones was synthesized on a preparative scale. The synthesis starts with a substituted 5-aminopyrazole that reacts with an isocyanate to give the corresponding urea. The latter undergoes a chlorotrimethylsilane-promoted [5+1] cyclocondensation with an aldehyde yielding the title pyrazolo[3,4-d]-4,5- dihydropyrimidin-6-one. Both synthetic steps are high-yielding (74-94%). The intermediates and the target compounds were isolated by simple crystallization. Ketones with the exception of isatin do not react with the open-chain urea intermediates.
INHIBITORS OF BIOFILM FORMATION OF GRAM-POSITIVE AND GRAM-NEGATIVE BACTERIA
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Page/Page column 46-47; 53, (2009/07/18)
The present invention relates to the use of compounds as broad spectrum inhibitors of bacterial biofilm formation. In particular the invention refers to a family of compounds that block the quorum sensing system of Gram-negative and Gram-positive bacteria, a process for their manufacture, pharmaceutical compositions containing them and to their use for the treatment and prevention of bacterial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.