Výsledky vyhledávání - "Cesarino Balsamini"

Synthesis of new C-6 alkyliden penicillin derivatives as β-lactamase inhibitors

Autor: W Baffone, Andrea Tontini, Cesarino Balsamini, E. Di Modugno, B. Di Giacomo, Francesca Bartoccini, Annalida Bedini, Giuseppe Gatti, A Felici, Giorgio Tarzia

Publikováno v: Il Farmaco. 57:273-283

New penicillin, penicillin sulfone and sulfoxide derivatives bearing a C-6-alkyliden substituent were prepared. Their chemical synthesis, in vitro antibacterial activity and inhibition properties against two selected enzymes representing Class A and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81934f6bf24ae5788ad4fbd516d47709
https://doi.org/10.1016/s0014-827x(02)01207-7

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2-N-Acylaminoalkylindoles: Design and Quantitative Structure−Activity Relationship Studies Leading to MT2-Selective Melatonin Antagonists

Autor: Marilou Pannacci, Marco Mor, Franco Fraschini, Andrea Tontini, Gilberto Spadoni, Cesarino Balsamini, Silvia Rivara, Bojidar Stankov, Valeria Lucini, Pier Vincenzo Plazzi, Giorgio Tarzia, Giuseppe Diamantini, Romolo Nonno

Publikováno v: Journal of Medicinal Chemistry. 44:2900-2912

Several indole analogues of melatonin (MLT) were obtained by moving the MLT side chain from C(3) to C(2) of the indole ring. Binding and in vitro functional assays were performed on cloned human MT1 and MT2 receptors, stably transfected in NIH3T3 cel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a09e37163e3860457e3d82ad01d28c89
https://doi.org/10.1021/jm001125h

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A new melatonin receptor ligand with mt1-agonist and MT2-antagonist properties

Autor: Cesarino Balsamini, Romolo Nonno, Assunta Croce, Gilberto Spadoni, Giorgio Tarzia, Marilou Pannacci, Bojidar Stankov, D. Esposti, Valeria Lucini, Franco Fraschini

Publikováno v: Journal of Pineal Research. 29:234-240

It has been difficult, so far, to obtain melatonin analogs possessing high selectivity for the respective melatonin receptors, mt 1 and MT 2 . In the present work, we report the synthesis and pharmacological characterization of a new compound N-{2-[5

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::2ec2a6dc29df4e96dc229fe9782a8f4c
https://doi.org/10.1034/j.1600-0633.2002.290406.x

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3-(2-Carbamoylvinyl)-4,5-dimethylpyrrole-2-carboxylic acids as ligands at the NMDA glycine-binding site: a study on the 2-carbamoylvinyl chain modification

Autor: Romano Di Fabio, Giorgio Tarzia, Giuseppe Diamantini, Gilberto Spadoni, Cesarino Balsamini, Andrea Tontini, Daniele Donati, Annalida Bedini

Publikováno v: Il Farmaco. 54:101-111

Twenty 4,5-dimethylpyrrole-2-carboxylic acids (5a-t) with different 2-carbamoylvinyl chains in position 3 were prepared to further investigate the relationships between structure and in vitro affinity for the strychnine-insensitive glycine-binding si

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::85e011f18ecb7db3cd7b0a452dd3e25c
https://doi.org/10.1016/s0014-827x(98)00110-4

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Melatonin Receptor Ligands: Synthesis of New Melatonin Derivatives and Comprehensive Comparative Molecular Field Analysis (CoMFA) Study

Autor: Claudia Silva, Giorgio Tarzia, Bojidar Stankov, Franco Fraschini, Giuseppe Diamantini, Silvia Rivara, Valeria Lucini, Gilberto Spadoni, Romolo Nonno, Cesarino Balsamini, Pier Vincenzo Plazzi, Marco Mor, Fabrizio Bordi

Publikováno v: Journal of Medicinal Chemistry. 41:3831-3844

The CoMFA methodology was applied to melatonin receptor ligands in order to establish quantitative structure-affinity relationships. One hundred thirty-three compounds were considered: they were either collected from literature or newly synthesized i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1d46ff6ac6e336824697f9d80320a38
https://doi.org/10.1021/jm9810093

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2-[N-Acylamino(C1−C3)alkyl]indoles as MT1 Melatonin Receptor Partial Agonists, Antagonists, and Putative Inverse Agonists

Autor: Marilou Pannacci, Bojidar Stankov, Giorgio Tarzia, Giuseppe Diamantini, Cesarino Balsamini, B. Di Giacomo, Marco Mor, Romolo Nonno, Valeria Lucini, Gilberto Spadoni, Silvia Rivara, A. Tontini, Annalida Bedini, Franco Fraschini, Pier Vincenzo Plazzi

Publikováno v: Journal of Medicinal Chemistry. 41:3624-3634

The synthesis of several novel indole melatonin analogues substituted at the 2-position with acylaminomethyl (8-11), acylaminoethyl (5a-k), or acylaminopropyl (13) side chains is reported. On the basis of a novel in vitro functional assay (specific b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f1f1cc09f293562bda3888f55b7eb93
https://doi.org/10.1021/jm970721h

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(E)-3-(2-(N-Phenylcarbamoyl)vinyl)pyrrole-2-carboxylic Acid Derivatives. A Novel Class of Glycine Site Antagonists

Autor: Giuseppe Diamantini, G. Tarzia, Gilberto Spadoni, Angelo Reggiani, R. Di Fabio, A. Feriani, A. Tontini, A. Bedini, R. Valigi, Giovanna Tedesco, Cesarino Balsamini

Publikováno v: Journal of Medicinal Chemistry. 41:808-820

The synthesis and preliminary biological evaluation of novel (E)-3-(2-(N-phenylcarbamoyl)-vinyl)pyrrole-2-carboxylic acids bearing alkyl, acyl, alkoxy, phenyl, and halo substituents at the 4- and 5-positions of the pyrrole ring are reported. These co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed84f5b87affc608866b2e49317c6e02
https://doi.org/10.1021/jm970416w

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Synthesis of 1-(isoxazol-3-yl)triazene derivatives. Antimetastatic activity of 3,3-dimethyl-1-(5-methylisoxazol-3-yl)triazene

Autor: G. Tarzia, Giuseppe Diamantini, L Perissin, Cesarino Balsamini, Valentina Rapozzi, A. Tontini

Publikováno v: European Journal of Medicinal Chemistry. 31:735-740

Summary The synthesis of some 3,3-dialkyl-1-(isoxazol-3-yl)triazenes is reported, together with preliminary biological tests on 3,3-dimethyl-1-(5-methylisoxazol-3-yl)triazene 3a . This compound exerts a selective antimetastatic action in mice bearing

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::535bdf7e7f202ab6d36d4ac939a729ec
https://doi.org/10.1016/0223-5234(96)85884-3

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Substituent effects on 1,3-dipolar cycloadditions to some 1,1-diphenyl-2-aza-1,3-butadiene derivatives

Autor: Marina Burdisso, Anna Maria Capelli, Cesarino Balsamini, Gilberto Spadoni, Annalida Bedini

Publikováno v: Tetrahedron. 50:3773-3784

The reactivity and in particular the siteselectivity of [3+2] electrocyclic additions to 1,1-diphenyl-2-aza -1,3-butadienes, substituted or not on the terminal carbon with methyl and phenyl, and with a 3-carbomethoxyl group, have been investigated wi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c58998f740a6d8ea03076ece73451f16
https://doi.org/10.1016/s0040-4020(01)90397-7

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Reactions of 3-carbomethoxy-2-aza-1,3-butadiene derivatives with dienophiles

Autor: M. Hamdan, Gilberto Spadoni, Annalida Bedini, Cesarino Balsamini, Giorgio Tarzia, Roberta Galarini

Publikováno v: Tetrahedron. 50:12375-12394

The reactions of 1,1-diphenyl-3-carbomethoxy-2-aza-1,3-butadiene derivatives la - e (on C4 : H,H or H,CH 3 or H,C 6 H 5 , both E and Z isomers), and of the C4 unsubstituted 1 -phenyl-1-ethoxy analogue 2, were studied with a number of electron-rich an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::571301a398016a6cbd3e496cc056c5d6
https://doi.org/10.1016/s0040-4020(01)89546-6

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