SPARATORE , Fabio

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A set of N-homolupinanoyl- and N-(v-lupinylthio)alkanoyl derivatives of tricyclic systems (as phenothiazine, iminodibenzyl and dihydropyridobenzodiazepinone) has been prepared and tested for affinity for rat muscarinic M1 and M2 receptor subtypes labeled with [3H]pirenzepine and [3H]AF-DX 384. Good affinity for both M1 and M2 subtypes was...

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...

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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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Fifteen quinolizidine derivatives have been tested for antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig (gp) heart tissues and to assess calcium antagonist activity. All compounds exhibited from moderate to high antiarrhythmic activity, and five of them (3, 4, 6, 13, and 15) were more active and potent than the...

A set of novel riminophenazine derivatives has been synthesized and evaluated for in vitro activity against chloroquine-sensitive (CQ-S) and chloroquine-resistant (CQ-R) strains of Plasmodium falciparum and against different species of Leishmania promastigotes. Most of the new compounds inhibited the growth of Leishmania promastigotes as well...

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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On the pattern of the potent and selective butyrylcholinesterase (BChE) inhibitors ethopropazine and Astra1397, sets of quinolizidinyl derivatives of bi- and tricyclic (hetero)aromatic systems were studied as dual, or BChE-selective inhibitors. All compounds exhibited activity against both cholinesterases, but inhibition of BChE was generally...

A library of 64 benzotriazole derivatives (17 of which were [4-(benzotriazol-2-yl)phenoxy]alkanoic acids) were screened for antiviral activity against a panel of twelve DNA and RNA viruses. Twenty-six compounds (12 of which were [4-(benzotriazol-2-yl)phenoxy]alkanoic acids) displayed activity against one or more viruses. CVB-5, RSV, BVDV, Sb-1...

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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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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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