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315 results on '"Da Settimo, F."'

2. Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors

Author

Nuti E., Casalini F., Santamaria S., Gabelloni P., Bendinelli S., Da Pozzo E., Costa B., MARINELLI, LUCIANA, LA PIETRA, VALERIA, NOVELLINO, ETTORE, Margarida Bernardo M., Fridman R., Da Settimo F., Martini C., Rossello A., Nuti, E., Casalini, F., Santamaria, S., Gabelloni, P., Bendinelli, S., Da Pozzo, E., Costa, B., Marinelli, Luciana, LA PIETRA, Valeria, Novellino, Ettore, Margarida Bernardo, M., Fridman, R., Da Settimo, F., Martini, C., and Rossello, A.

Published
2011

4. Identification of anxiolytic/non sedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the GABAA alfa2 benzodiazepine receptor

Author

Taliani S., Da Settimo F., Marini A. M., La Motta C., Simorini F., Salerno S., Cosconati S., Salvetti F., L’Abbate G., Trasciatti S., Montali M., Costa B., Martini C., COSIMELLI, BARBARA, NOVELLINO, ETTORE, GRECO, GIOVANNI, MARINELLI, LUCIANA, Taliani, S., Cosimelli, Barbara, Da Settimo, F., Marini, A. M., La Motta, C., Simorini, F., Salerno, S., Novellino, Ettore, Greco, Giovanni, Cosconati, S., Marinelli, Luciana, Salvetti, F., L’Abbate, G., Trasciatti, S., Montali, M., Costa, B., and Martini, C.

Published
2009

6. 2-Phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one derivatives as a new class of adenosine receptor antagonists

Author

Primofiore G., Da Settimo F., Taliani S., Sergianni V., Simorini F., La Motta C., Marini A. M., Tuscano D., Martini C., GRECO, GIOVANNI, COSIMELLI, BARBARA, NOVELLINO, ETTORE, Ettmayer P., Eckert G., Primofiore, G., Da Settimo, F., Taliani, S., Sergianni, V., Simorini, F., La Motta, C., Marini, A. M., Tuscano, D., Martini, C., Greco, Giovanni, Cosimelli, Barbara, and Novellino, Ettore

Subjects
heterocycles, antagonist, adenosine receptor
Published
2005

11. Synthesis of 3-(2'-Furoyl)indole Derivatives as Potential New Ligands at the Benzodiazepine Receptor, Structurally More Restrained Analogues of Indoleglyoxylylamides

Author

Da Settimo, A., Primofiore, G., Da Settimo, F., Marini, A. M., Novellino, E., Greco, G., Martini, C., Senatore, G., ANTONIO LUCACCHINI, DA SETTIMO, A., Primofiore, G., DA SETTIMO, F., Marini, A. M., Novellino, Ettore, Greco, Giovanni, Martini, C., Senatore, G., and Lucacchini, A.

Subjects
Models, Molecular, Indoles, Animals, Cattle, Furans, Ligands, Receptors, GABA-A
Abstract

A number of furoylindoles were synthesized with the aim of obtaining structurally more restrained analogues of the previously described indoleglyoxylylamides, which are high affinity ligands at the benzodiazepine receptor. In these new compounds, the oxygen atom of the oxalyl CO(2) is inserted into the rigid furan ring. However, unlike the glyoxylylamides, they proved to be incapable of interacting with the benzodiazepine receptor. To rationalize these results, molecular electrostatic potentials were calculated; these indicated a positive electrostatic potential region for the furan oxygen, which thus prevents the formation of a hydrogen bond necessary for interaction with the receptor. Nevertheless, these findings confirmed that the CO(2) of the indoleglyoxylylamide derivatives represents one of the principal points of interaction with the receptor site for these kinds of ligands, as previously hypothesized by us.

Published
1995

12. Pharmacological characterization of a new Ca2+ sensitizer

Author

Dorigo, P., Floreani, M., Santostasi, G., Maragno, I., Danieli-Betto, D., Germinario, E., Magno, S. M., Primofiore, G., Anna Maria Marini, and Da Settimo, F.

Subjects
Male, Dose-Response Relationship, Drug, Sarcoplasmic Reticulum Ca2+Release, Papillary Muscle, calcium sensitivity, Guinea Pigs, Imidazoles, Myocardial Contraction, Caffeine, Animals, Benzimidazoles, Calcium, Muscle Contraction
Abstract

The benzimidazole molecule was modified to synthesize a Ca(2+) sensitizer devoid of additional effects associated with Ca(2+) overload. Newly synthesized compounds, termed 1, 2, 3, 4, and 5, were evaluated in spontaneously beating and electrically driven atria from reserpine-treated guinea pigs. Compound 3 resulted as the most effective positive inotropic agent, and experiments were performed to study its mechanism of action. In spontaneously beating atria, the inotropic effect of 3 was concentration-dependent (3.0 microM-0.3 mM). Compound 3 was more potent and more active than the structurally related Ca(2+) sensitizers sulmazole and caffeine, but unlike them it did not increase the heart rate. In electrically driven atria, the inotropic activity of 3 was well preserved and it was not inhibited by propranolol, prazosin, ranitidine, pyrilamine, carbachol, adenosine deaminase, or ruthenium red. At high concentrations (0.1-1.0 mM) 3 inhibited phosphodiesterase-III, whereas it did not affect Na(+)/K(+)-ATPase, sarcolemmal Ca(2+)-ATPase, Na(+)/Ca(2+) exchange carrier, or sarcoplasmic reticulum Ca(2+) pump activities of guinea pig heart. In skinned fibers obtained from guinea pig papillary muscle and skeletal soleus muscle, compound 3 (0.1 mM, 1 mM) shifted the pCa/tension relation curve to the left, with no effect on maximal tension and no signs of toxicity. Compound 3 did not influence the basal or raised tone of guinea pig isolated aorta rings, whose cells do not contain the contractile protein troponin. The present results indicate that the inotropic effect of compound 3 seems to be primarily sustained by sensitization of the contractile proteins to Ca(2+).

Published
2000

44. Synthesis of pyrimido1,2abenzimidazol410Hone derivatives and evaluation of their interactions with DNA

Author

Da Settimo, A., Primofiore, G., Da Settimo, F., Marini, A. M., Taliani, S., Salerno, S., and Dalla Via, L.

Abstract

The synthesis of new derivatives of the planar tricyclic pyrimido1,2abenzimidazole system featuring protonable side chains in the 3 andor 10 positions is described. The reported literature procedures for the preparation of the intermediate 3ethoxycarbonylpyrimido1,2abenzimidazol410Hone 15, starting from 2aminobenzimidazole 18and diethyl ethoxymethylenemalonate, were revised. The interaction with DNA, the intrinsic binding constants, and the antiproliferative activity of a number of compounds 1–8, 10, 11 were preliminarly investigated.

Published
2003
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46. Synthesis and evaluation of aminoadamantane derivatives for in vitro anti-HIV and antitumor activities

Author

Da Settimo, A., Anna Maria Marini, Primofiore, G., and Da Settimo, F.

Subjects
Molecular Structure, Drug Evaluation, Preclinical, Tumor Cells, Cultured, HIV, Humans, Adamantane, Antineoplastic Agents, Benzimidazoles, Drug Screening Assays, Antitumor, Antiviral Agents, Cell Line
Abstract

The synthesis of a series of 2-aminobenzimidazole and indole amide derivatives containing the adamantyl moiety is described. The compounds, evaluated for in vitro anti-HIV and antitumor activities, were found to be moderately active or inactive, versus drug-treated controls, used for comparison purposes.

49. Synthesis and local anaesthetic activity of some 7-amino-2-dialkylaminoalkylpyrrolo[3,4-c]pyridine derivatives

Author

Da Settimo F, Am, Marini, La Motta C, Simorini F, Luchetti E, and Simone Bertini

Subjects
Male, Solubility, Pyridines, Animals, Rabbits, Anesthetics, Local
Abstract

A number of 7-amino-2-dialkylaminoalkylpyrrolo[3,4-c] pyridin-1,3(2H)-dione derivatives were synthesized and their local anaesthetic activity was evaluated in vivo by corneal anaesthesia in rabbits. Only compounds 3,9 and 14 showed any activity, albeit lower than that of the reference drug lidocaine.

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