NOVELLI , Federica

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As analogues of some conformationally restricted spiropiperidine derivatives which are endowed with high affinity for σ1 receptor, a set of 16 spiro[1,2,4-benzotriazine-3(4H),4'-(1'-substituted)piperidines] and congeneric compounds was prepared and tested for affinity to σ1 receptor subtype. All N-arylalkyl substituted derivatives exhibited...

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A small set of 9-(lupinylthio)xanthene, -thioxanthenes and α-(lupinylthio)diphenylmethanes was prepared and found to inhibit the angiotensin II-induced contractions of guinea pig ileum. Some of these compounds were also moderately active in vitro as tracheal relaxants and one compound was more active than aspirin against arachidonic...

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Six triorganotin derivatives of thiolupinine(1-mercaptolupinane), 2-mercaptobenzoxazole and 2-mercaptobenzothiazole were prepared and tested against several bacteria, fungi and protozoa. Most compounds exhibited high activity against the tested microorganisms and particularly worth noting was the activity of triethyltin lupinylsulfide on...

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Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)- thioacetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subtypes. During the synthesis...

Seven gold complexes were prepared and investigated for biocidal activity against Gram-positive and -negative bacteria, fungi and protozoa. All of them were active against the tested microorganisms with the exception of Pseudomonas aeruginosa. In many cases minimum inhibitory concentrations (MIC) were well below 1 μg:ml. The activity is not...

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Respiratory syncytial virus (RSV) has been identified as a main cause of hospitalisation in infants and children. To date, the current therapeutic arsenal is limited to ribavirin and palivizumab with variable efficacy. In this work, starting from a number of in-house series of previously described anti-RSV agents based on the benzimidazole...

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We tested the efficacy of novel cyclooxygenase 2 (COX-2) inhibitors in counteracting glia-driven neuroinflammation induced by the amyloidogenic prion protein fragment PrP90-231 or lipopolysaccharide (LPS). In search for molecules with higher efficacy than celecoxib, we focused our study on its 2,3-diaryl-1,3-thiazolidin-4-one analogues. As...