Výsledky vyhledávání - "Giancarlo Merlo"

Discovery and structure–activity relationship of a novel spirocarbamate series of NPY Y5 antagonists

Autor: Jonathan Mark Bentley, Matteo Biagetti, Laura Caberlotto, Colin Philip Leslie, Romano Di Fabio, Thorsten Genski, Daniele Donati, Laura Zonzini, Catia Seri, Sebastien Guery, Stefania Contini, Angelica Mazzali, Domenica Antonia Pizzi, Michela Tessari, Giancarlo Merlo, Fabiola Sacco

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:6103-6107

A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5]decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine sub-nanomolar Y5 activity with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f760c980840d16f98ad0723ece4796f8
https://doi.org/10.1016/j.bmcl.2010.08.041

Zobrazit plný text záznamu

Ocular hypotensive efficacy and safety of travoprost 0.004% in inadequately controlled primary open-angle glaucoma or ocular hypertension: short-term, multicenter, prospective study

Autor: Alessandro David, Giuseppe Trabucchi, Roberto Ratiglia, Gemma Caterina Maria Rossi, Rosella Radaelli, Maria R. Curatola, Giancarlo Merlo, Mirella Blini

Publikováno v: Current Medical Research and Opinion. 25:57-63

To evaluate the intraocular pressure (IOP) lowering efficacy and safety of travoprost 0.004% in patients with open-angle glaucoma or ocular hypertension, poorly controlled with or intolerance to beta-blockers. To record the short-term effect on diast

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25d784f792adfbf4969e69170f020a1f
https://doi.org/10.1185/03007990802569315

Zobrazit plný text záznamu

Novel 5-HT1A/1B/1D receptors antagonists with potent 5-HT reuptake inhibitory activity

Autor: Halina T Serafinowska, Claire M. Scott, Jeannette M. Watson, Kathryn R. Starr, Peter J. Lovell, Giancarlo Merlo, Frank E. Blaney, Paul W. Smith

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5581-5585

Novel 2-methyl-5-quinolinyl-1-piperazinylalkyl-3,4-dihydro-2H-1,4-benzoxazin-3-ones showing high affinities for the 5-HT1A/1B/1D receptors coupled with potent 5-HT reuptake inhibitory activity have been discovered. This is the first report describing

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::18a37202e909d0db16f37c7cbfa2751d
https://doi.org/10.1016/j.bmcl.2008.08.110

Zobrazit plný text záznamu

6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors

Autor: Alessia Vesentini, Luigi Piero Stasi, Barbara Bertani, Matthew Hill, Jeannette M. Watson, Steven Mark Bromidge, Enrica Granci, Laura Zonzini, Valeria Zucchelli, Howard Robert Marshall, Stefania Faedo, Giancarlo Merlo, Laurie J. Gordon, Manuela Borriello

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 18:5653-5656

Investigation of a series 6-[2-(4-aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones has led to the discovery of potent 5-HT(1A/1B/1D) receptor antagonists with and without additional SerT affinity. Modulation of the different target activities g

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c4ec2dc4e71739fadb1945c9d406597
https://doi.org/10.1016/j.bmcl.2008.08.084

Zobrazit plný text záznamu

Deprotection of o-Nitrobenzensulfonyl (Nosyl) Derivatives of Amines Mediated by a Solid-Supported Thiol

Autor: Giancarlo Merlo, Maurizio Taddei, Margherita Salaris, Alfredo Paio, Daniele Donati, Francesca Cardullo

Publikováno v: Synlett. 2005:2996-2998

A new protocol based on a solid-supported thiol was developed for high yielding deprotection of o-nitrobenzensulfonyl amides derived from primary and secondary amines. The reaction can be carried out at room temperature for 24 hours or accelerated by

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b30d6d262b999092adc190ae023b29e9
https://doi.org/10.1055/s-2005-921892

Zobrazit plný text záznamu

5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors

Autor: Angela Bridges, Gang Yao, Geoffrey J. Cutler, Paul Bamborough, Svetlana L. Belyanskaya, Caroline Brough, Gabriella Gentile, Benjamin D. Bax, Margarete Neu, Aaron Coffin, Giancarlo Merlo, Paul S. Carter, Giovanni Bernasconi, Alfonso Pozzan

Publikováno v: Bioorganicmedicinal chemistry letters. 22(5)

5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5b66eb76e81f7b2c32b4bb452fbb6ccb
https://pubmed.ncbi.nlm.nih.gov/22310227

Zobrazit plný text záznamu

Identification of 2-(4-pyridyl)thienopyridinones as GSK-3β inhibitors

Autor: Giancarlo Merlo, Geoffrey J. Cutler, Paul S. Carter, Caroline Brough, Mia Takada, Paul Bamborough, Margarete Neu, Giovanni Bernasconi, Paola Marzorati, Gabriella Gentile, Angela Bridges, Alfonso Pozzan, Benjamin D. Bax

Publikováno v: Bioorganicmedicinal chemistry letters. 21(16)

The discovery of a novel series of 2-(4-pyridyl)thienopyridinone GSK-3β inhibitors is reported. X-ray crystallography reveals its binding mode and enables rationalization of the SAR. The initial optimization of the template for improved cellular act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::02fe34864e458e7407cbe75474f96a64
https://pubmed.ncbi.nlm.nih.gov/21764580

Zobrazit plný text záznamu

Novel spirotetracyclic zwitterionic dual H(1)/5-HT(2A) receptor antagonists for the treatment of sleep disorders

Publikováno v: Journal of medicinal chemistry. 53(21)

Histamine H(1) and serotonin 5-HT(2A) receptors mediate two different mechanisms involved in sleep regulation: H(1) antagonists are sleep inducers, while 5-HT(2A) antagonists are sleep maintainers. Starting from 9'a, a novel spirotetracyclic compound

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f441b5897e4354fcfc1d72f68a14507c
https://pubmed.ncbi.nlm.nih.gov/20942472

Zobrazit plný text záznamu

Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists

Autor: Romano Di Fabio, Laura Zonzini, Giancarlo Merlo, Silvia Tomelleri, Alfredo Paio, Paola Zarantonello, Adelheid Roth, Federica Tonelli, Anna Maria Capelli, Angelo Giacometti, Elisa Moro, Emilio Merlo-Pich, Fabrizio Micheli

Publikováno v: Bioorganicmedicinal chemistry letters. 20(24)

A new class of selective NPS antagonist was developed starting from a commercially available product identified by screening activities. Experimental NMR observations and computational experiments allowed the discovery of a new class of derivatives.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f6848d18f251e64f68c742317e1734f
https://pubmed.ncbi.nlm.nih.gov/21055936

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání