1,721,077 research outputs found
Adenosine A1 modulators: a patent update (2008 to present)
No full textIntroduction: In 2008, we published our review titled 'Therapeutic potential of A1 adenosine receptor ligands - a survey of recent patent literature' that reported the compounds active on A1 adenosine receptors (ARs) and the applications of A1 AR ligands patented in the period 2005 - 2008. Areas covered: This article is a discussion of the patents about the same subjects, issued in the period 2008 to present. It is organized similarly to the first one, with a section about new compounds, subdivided on the basis of their functional activity (agonists, antagonists and allosteric modulators) and a section regarding new therapeutic applications. Expert opinion: The main novelty is represented by the patenting of A1 AR ligands with dual selectivity which may show, in some conditions, better efficacy and fewer side effects. Moreover, while the way to arrive into the market appears full of obstacles for selective A1 ligands that need systemic administration for long-term therapy, better chances are foreseen in applications requiring topical administration
THERAPEUTIC POTENTIAL OF A1 ADENOSINE RECEPTOR LIGANDS: A SURVEY OF RECENT PATENT LITERATURE
No full textIn recent years, a number of companies, universities and other institutions have invested in research on new molecules acting as agonists, antagonists and enhancers on A1 adenosine receptors (ARs) and in the evaluation of their new therapeutic applications. Objective: To review recent patenting activity on this topic. Methods: The first part of this article describes the compounds patented, subdivided by functional activity, and the second part the most relevant therapeutic applications or new uses for A1 AR ligands, with a focus on compounds in or soon to be in clinical trials. Conclusion: Although a number of potential therapeutic applications are proposed in the recent literature, at present, in the authors’ opinion, very few A1 ligands are close to coming on the market, probably due to limited selectivity towards the target tissue or organ
8-Azapurine nucleus: a versatile scaffold for different targets
No full text8-Azapurine nucleus is a bioisoster of the purine nucleus. Variously substituted 8-azapurines have been synthesised and studied for their interactions with many enzymes and receptors and for their antitumor and antiviral activity. In this paper the main results of the studies made in these last years
on this topic are reported
An initial comparison of the content of bitter substances in Cynara Scolymus L. plants obtained from rooted of shoots and micropropagation
No full textCynaropicrin, a sesquiterpene, is the main bitter compound in globe artichoke and is important for the organolectic and nutritional quality of the fresh product and leaf extracts. Artichoke plants of the late variety "Grato 1" obtained from rooted offshoots and by micropropagation were compared with respect to the bitter content in the young leaves and heads. The bitter content, expressed as cynaropicrin (% of dry weight), was determined by an alkalimetric method. The results show a bitter content ranging from 6.82 to 9.63%; the leaves of the micropropagated plants had 29% less bitter content than the plants traditionally propagated by rooted offshoots
Antimicrobial properties of flavonoids.
No full textFlavonoids are a class of plant constituents that have received increasing interest over the last decades. This chapter deals with the antimicrobial activity of some natural flavonoids or extracts rich in these constituents reported in the literature during the last five years. An introduction explains the chemical structure of this class of natural compounds, their biosynthesis, plant sources and health benefits. Then the most significant articles from the scientific literature are reported, divided into two sections: studies on flavonoids with antibacterial and antifungal activities, respectively. In each paragraph we have listed the papers according to the chemical complexity of the flavonoid structures, from the simplest to the most complex ones, both aglicones and glycosides and often gathering together the articles according to the main microbial target. A paragraph on the antimicrobial activity of combination of different flavonoids or between flavonoids and antibiotics (synergic effect) is also present. For many of the flavonoids cited the MIC values of their activity have also been reported. Chemical structures of the majority of the compounds cited in the chapter are pictured in figures; tables have been compiled summarising the most important information reported in this chapter
Modification of the 1,2,3-Triazole Ring Present in an Effective in vitro Inhibitor of Prostaglandin Synthesis
No full text1,2,3-Triazolo[4,5-d]-1,2,4-triazolo[4,3-b]pyridazines
No full textSome new 1,2,3-triazolo[4,5-d]-1,2,4-triazolo[4,3-b]pyridazines were prepared starting from the corresponding 1,2,3-triazolo[4,5-d]pyridazines via the formation of the 1,2,4-triazole ring, by condensation of an appropriate monocarbon fragment with the 4-hydrazino substituent and the nitrogen atom in the 5 position of the heterocycle. Condensation of 4-phenylhydrazino substituted derivatives with formic acid gave zwitterionic compounds
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