Papers by Fabio Sparatore
PubMed, Aug 1, 1997
A set of benzimidazole derivatives bearing on position 2 a tetrahydropyranyl or tetrahydrofuranyl... more A set of benzimidazole derivatives bearing on position 2 a tetrahydropyranyl or tetrahydrofuranyl residue was prepared and tested for antitumoral, anti HIV-1 and other pharmacological activities. While the anti-HIV activity was completely lacking, moderate antitumoral activity was found in a few compounds; particularly the 5,6-dichloro-2-(tetrahydropyran-2-yl)-benzimidazole (8) was able to inhibit the growth of 19 cell lines of humane tumors at near micromolar concentration. On the other hand compounds 4, 6-8 and 10 exhibited significant tracheal relaxant activity in vitro at concentration 3-10 micrograms/ml, thus resulting superior to theophylline and comparable to amrinone.
Farmaco, Jul 1, 1999
Thirty-one N-derivatives of cytisine were prepared in order to modify its pharmacological profile... more Thirty-one N-derivatives of cytisine were prepared in order to modify its pharmacological profile and to obtain compounds of potential therapeutic interest either at a peripheral or central level, particularly as nicotinic ligands with improved ability to cross the blood–brain barrier. Actually, with the introduction of different kinds of substituent on the basic nitrogen of cytisine a variety of activities were
Chemischer Informationsdienst, Jan 13, 1981
Farmaco, Apr 1, 2001
Thirteen [(aryl/heteroaryl-piperazinyl)alkyl]benzotriazoles were prepared as potential trazodone-... more Thirteen [(aryl/heteroaryl-piperazinyl)alkyl]benzotriazoles were prepared as potential trazodone- and buspirone-like drugs. The synthesized compounds displayed from moderate to good affinity to the serotonin 5-HT1A receptor and only modest or poor affinity to the dopamine D2 receptor, similar to buspirone. The introduction of substituents on the benzotriazole ring did not improve the affinity to the 5-HT1A receptor, compared to the previously described
PubMed, Aug 1, 1997
Sets of benzimidazole and benzotriazole derivatives bearing on position 1 or 2 a tetrahydrofurany... more Sets of benzimidazole and benzotriazole derivatives bearing on position 1 or 2 a tetrahydrofuranyl or tetrahydropyranyl moieties were prepared through the addition of the suitable benzazoles on 2,3-dihydrofuran and 3,4-dihydro-2H-pyran. The reactions were carried on either without solvent or in carbon tetrachloride solution. In the last case some peculiar chlorinated side products were isolated and characterized. Twenty compounds were screened for in vitro antitumoral and anti-HIV-1 activities and found poorly active or completely inactive. On the other hand several compounds exhibited good tracheal relaxant activity in vitro; compound 8, 11, 16, 24 and 26 resulted more active than theophylline in this test, while compound 11 was comparable to amrinone till the concentration of 3 micrograms/ml. Finally, compound 5 resulted endowed with a strong diuretic and saluretic activity at the dose of 3 mg/Kg, thus representing a new lead for discovering new diuretic agents.
Chemischer Informationsdienst, Jan 15, 1980
PubMed, Mar 1, 1992
Several compounds possessing imidazo[4,5-b]pyridine and benzimidazole structure bearing substitue... more Several compounds possessing imidazo[4,5-b]pyridine and benzimidazole structure bearing substituents in position 2 were prepared in order to evaluate an anti-ulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole. Among sixteen compounds taken as representatives of the synthetised series only one (3d) showed a good activity by i.m. administration at 50 mg/kg, while by oral administration of 100 mg/kg a certain number was active and in some cases this activity was quite superior to that of omeprazole.
PubMed, Jun 1, 1975
In order to improve the analgesic and antiarrhythmic activities of 1-dialkylaminoalkyl-2-benzotri... more In order to improve the analgesic and antiarrhythmic activities of 1-dialkylaminoalkyl-2-benzotriazolylmethylbenzimidazoles previously described, forty derivatives with a chlorine, trifluoromethyl, acetyl or nitrogroup in 5 position were prepared.
Chemischer Informationsdienst, Aug 22, 1972
Chemischer Informationsdienst, Jul 25, 1972
ChemInform, Aug 19, 2010
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
PubMed, Sep 1, 1993
Twenty compounds possessing benzimidazole, imidazo[4,5-b]pyridine and quinoxaline structure beari... more Twenty compounds possessing benzimidazole, imidazo[4,5-b]pyridine and quinoxaline structure bearing either a substituted arylmethylmercapto- or an arylmethylsulfinyl group in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole at the dose of 50 mg/kg after i.m. administration. One third of these compounds showed a moderate activity, being about half potent as omeprazole.
Chemischer Informationsdienst, Aug 1, 1972
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Papers by Fabio Sparatore