Výsledky vyhledávání - "Claudio Biancalani"

Synthesis and inverse virtual screening of new bi-cyclic structures towards cancer-relevant cellular targets

Autor: Letizia Crocetti, Giuseppe Floresta, Shabnam Nazir, Claudia Vergelli, Amrit Bhogal, Claudio Biancalani, Nicoletta Cesari, Maria Paola Giovannoni, Agostino Cilibrizzi

We report here synthetic approaches to access new classes of small molecules based on three heterocyclic scaffolds, i.e. 3,7-dihydropyrimido[4,5-d]pyridazine-4,8-dione, 1,8-naphthyridin-4(1H)-one and 4H-pyrido[1,2-a]pyrimidin-4-one. The bi-cyclic str

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ecc18cb64d9be088c0a525a92a73b54
http://hdl.handle.net/20.500.11769/538011

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Synthesis and evaluation as PDE4 inhibitors of pyrimidine-2,4-dione derivatives

Autor: Claudia Vergelli, Marta Nesi, Agostino Cilibrizzi, Letizia Crocetti, Nicoletta Cesari, Vittorio Dal Piaz, Claudio Biancalani, Maria Paola Giovannoni, Rosanna Matucci, Alessia Graziano

Publikováno v: Drug Development Research. 72:274-288

A series of nitraquazone analogs with a pyrimidindione core was synthesized and tested for inhibitory activity on PDE4, selectivity versus PDE3 and PDE5 and for affinity towards the rolipram high-affinity binding site (HARBS). The 5-anilino derivativ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6aaf18c8c2ec8899ef6408c9814a191e
https://doi.org/10.1002/ddr.20395

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4-Amino-5-substituted-3(2H)-pyridazinones as Orally Active Antinociceptive Agents: Synthesis and Studies on the Mechanism of Action

Autor: Claudia Vergelli, Nicoletta Cesari, Pierfrancesco Biagini, Vittorio Dal Piaz, Carla Ghelardini, Claudio Biancalani, Alessia Graziano, E. Vivoli, Maria Paola Giovannoni

Publikováno v: Journal of Medicinal Chemistry. 50:3945-3953

A number of 4-amino-5-vinylpyridazinones and 4-amino-5-heterocyclic-pyridazinones were synthesized and tested for their analgesic activity. Many of these compounds, tested at doses of 3-20 mg kg-1 po, showed good antinociceptive activity, reducing by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6aa5d48c9c404c7be50f2c07b5c3455f
https://doi.org/10.1021/jm070161e

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Synthesis of pyrrolo[2,3-d]pyridazinones as potent, subtype selective PDE4 inhibitors

Autor: Pierfrancesco Biagini, Vittorio Dal Piaz, Claudio Biancalani, Claudia Vergelli, Nicoletta Cesari, Alessia Graziano, Maria Paola Giovannoni

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry. 22:309-318

A series of pyrrolo [2,3-d]pyridazinones was synthesized and tested for their inhibitory activity on PDE4 subtypes A, B and D and selectivity toward Rolipram high affinity binding site (HARBS). New agents with interesting profile were reported; in pa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::102c01bf97e6fb97c103110ca0664b13
https://doi.org/10.1080/14756360601114700

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ChemInform Abstract: Synthesis of New Tetracyclic Azaheteroaromatic Cores via Auto-Tandem Pd-Catalyzed and One-Pot Pd- and Cu-Catalyzed Double C-N Bond Formation

Autor: Claudio Biancalani, Joris W. De Schutter, Tom R. M. Rauws, Bert U. W. Maes

Publikováno v: ChemInform. 41

Inter- and intramolecular transition metal-catalyzed amination of 2-chloro-3-iodopyridine and 2,3-dibromopyridine, respectively, with benzodiazinamines yielded six hitherto unknown tetracyclic azaheteroaromatic cores. C–N bond formation was achieve

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f44919b9786ca928a17b0facf0977d32
https://doi.org/10.1002/chin.201052162

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Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands

Autor: Claudia Vergelli, Agostino Cilibrizzi, María Isabel Loza, Amadeu Gavaldà, María Isabel Cadavid, Letizia Crocetti, Alessia Graziano, Claudio Biancalani, Jose-Luis Diaz, Maria Paola Giovannoni, Vittorio Dal Piaz

Publikováno v: Bioorganicmedicinal chemistry. 18(22)

A series of pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones was synthesized and tested in radioligand binding assays to determine their affinities for the human adenosine A(1), A(2A), A(2B) and A(3) receptors. Results indicated that this scaff

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b454bf37c69d07436e21ded4df60a46
https://pubmed.ncbi.nlm.nih.gov/20937560

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Functionalized pyrazoles and pyrazolo[3,4-d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity

Autor: Daniele Spinabelli, Agostino Cilibrizzi, Elisabetta Armani, Claudia Vergelli, Pierfrancesco Biagini, Maria Paola Giovannoni, Paola Puccini, Andrea Rizzi, Paola Maria Gallo, Letizia Crocetti, Maurizio Delcanale, Nicoletta Cesari, Vittorio Dal Piaz, Claudio Biancalani, Paola Caruso, Alessia Graziano

Publikováno v: Bioorganicmedicinal chemistry. 18(10)

A series of pyrazoles and pyrazolo[3,4-d]pyridazinones were synthesized and evaluated for their PDE4 inhibitory activity. All the pyrazoles were found devoid of activity, whereas some of the novel pyrazolo[3,4-d]pyridazinones showed good activity as

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18c17bcb6c4c25b9004d92f31b3fadc2
https://pubmed.ncbi.nlm.nih.gov/20413313

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Further studies on arylpiperazinyl alkyl pyridazinones: discovery of an exceptionally potent, orally active, antinociceptive agent in thermally induced pain

Autor: Claudio Biancalani, Maria Paola Giovannoni, Nicoletta Cesari, Stefano Pieretti, Alessia Graziano, Agostino Cilibrizzi, Vittorio Dal Piaz, Giorgina Mangano, Lorenzo Polenzani, Amalia Di Gianuario, Mariantonella Colucci, Claudia Vergelli, Beatrice Garrone

Publikováno v: Journal of medicinal chemistry. 52(23)

A number of pyridazinone derivatives bearing an arylpiperazinylalkyl chain were synthesized and tested icv in a model of acute nociception induced by thermal stimuli in mice (tail flick). The most interesting and potent compound in this series was 6a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c392c0ba44dd0c5c4346ec371bc3201e
https://pubmed.ncbi.nlm.nih.gov/19788200

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6-methyl-2,4-disubstituted pyridazin-3(2H)-ones: a novel class of small-molecule agonists for formyl peptide receptors

Autor: Stefano Pieretti, Agostino Cilibrizzi, Liliya N. Kirpotina, Nicoletta Cesari, Igor A. Schepetkin, Marie Josephe Rabiet, Vittorio Dal Piaz, Mark T. Quinn, Claudio Biancalani, Jeff Holderness, Claudia Vergelli, Richard D. Ye, Maria Paola Giovannoni, Alessia Graziano

Publikováno v: Journal of medicinal chemistry. 52(16)

Following a ligand-based drug design approach, a potent mixed formyl peptide receptor 1 (FPR1) and formyl peptide receptor-like 1 (FPRL1) agonist (14a) and a potent and specific FPRL1 agonist (14x) were identified. These compounds belong to a large s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31f31bbf26a905585b5d5d10a5ce2f84
https://pubmed.ncbi.nlm.nih.gov/19639995

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