1,2,4-Triazolyl 5-Azaspiro[2.4]heptanes: Lead Identification and Early Lead Optimization of a New Series of Potent and Selective Dopamine D3 Receptor Antagonists

Autor: Aldo Feriani, Laura Zonzini, Laura Castelletti, Selena Nola, Michele Dal Cin, Teresa Semeraro, Sylvie Gehanne, Silvia Tomelleri, Filippo Visentini, Palmina Cavallini, Susanna Cremonesi, Annalisa Pellacani, Anna Sava, Alessia Bacchi, Andrea Wong, Simone Braggio, Luca Tarsi, Mahmud Kajbaf, Paolo Cavanni, Elisabetta Perdona, Christian Heidbreder, Luciano Marchiò, Beatrice Oliosi, Fabrizio Micheli

Publikováno v: Journal of Medicinal Chemistry. 59:8549-8576

A novel series of 1,2,4-triazolyl 5-azaspiro[2.4]heptanes with high affinity and selectivity at the dopamine (DA) D3 receptor (D3R) is described. Some of these compounds also have high selectivity over the hERG channel and were characterized with res

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e92639ff81d14ff2d424ab7f16b988a
https://doi.org/10.1021/acs.jmedchem.6b00972

Practical synthesis of novel purine analogues as Hsp90 inhibitors

Autor: Serena Pasquini, Fabrizio Manetti, Federico Corelli, Teresa Semeraro, Claudia Mugnaini

Publikováno v: Tetrahedron. 64:11249-11255

The development of a straightforward synthesis of 4-amino-6-benzyl-6 H -pyrrolo[3,4- d ]pyrimidine and 7-amino-2-benzyl-2 H -pyrazolo[4,3- d ]pyrimidine derivatives allowed for the preparation of a small family of potential Hsp90 inhibitors. Some of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3ee4625a372ea31e84c24bc6ed81cf1
https://doi.org/10.1016/j.tet.2008.09.030

Simplified Analogues of Immucillin-G Retain Potent Human Purine Nucleoside Phosphorylase Inhibitory Activity

Autor: Silvia Valensin, Maurizio Botta, Federico Corelli, Fabrizio Manetti, Teresa Semeraro, Andrea Lossani, Reinaldo Alvarez, Chiara Ghiron, Claudia Mugnaini, Federico Focher

Publikováno v: Journal of Medicinal Chemistry. 49:6037-6045

A set of deazaguanine derivatives 1-3 targeting human purine nucleoside phosphorylase (hPNP) have been designed and synthesized. The new compounds are characterized by the presence of a structurally simplified "azasugar" motif to be more easily acces

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40a8fae9c1ffbf6eabdf2c507082e550
https://doi.org/10.1021/jm060547+

Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands

Autor: Francesca Guida, Lavinia Cicione, Federico Corelli, Claudia Mugnaini, Roger G. Pertwee, Teresa Semeraro, Maria De Chiaro, Serena Pasquini, Livio Luongo, Vincenzo Di Marzo, Daniele Bolognini, Maria Grazia Cascio, Sabatino Maione, Pietro Marini, Maria Cristina De Rosa, Alessia Ligresti

Publikováno v: Journal of medicinal chemistry 53 (2010): 5915–5928.
info:cnr-pdr/source/autori:Pasquini S, Ligresti A, Mugnaini C, Semeraro T, Cicione L, De Rosa M, Guida F, Luongo L, De Chiaro M, Cascio MG, Bolognini D, Marini P, Pertwee R, Maione S, Di Marzo V, Corelli F./titolo:Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands./doi:/rivista:Journal of medicinal chemistry/anno:2010/pagina_da:5915/pagina_a:5928/intervallo_pagine:5915–5928/volume:53

A set of quinolone-3-carboxamides 2 bearing diverse substituents at position 1, 3, and 6 of the bicyclic nucleus was prepared. Except for six compounds exhibiting Ki > 100 nM, all the quinolone-3-carboxamides 2 proved to be high affinity CB2 ligands,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f731f5ff70ab14c9c6058d123b03fb17
https://pubmed.ncbi.nlm.nih.gov/20718492

Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 3. Synthesis, Structure−Affinity Relationships, and Pharmacological Characterization of 6-Substituted 4-Quinolone-3-carboxamides as Highly Selective Cannabinoid-2...

Autor: Serena Pasquini, Alessia Ligresti, Claudia Mugnaini, Teresa Semeraro, Lavinia Cicione, Maria De Rosa, Francesca Guida, Livio Luongo, Maria De Chiaro, Maria Grazia Cascio, Daniele Bolognini, Pietro Marini, Roger Pertwee, Sabatino Maione, Vincenzo Di Marzo, Federico Corelli

Publikováno v: Journal of Medicinal Chemistry; Aug2010, Vol. 53 Issue 16, p5915-5928, 14p