Výsledky vyhledávání - "Nicholas J. S. Harmat"

Discovery of a New Series of Potent and Selective Linear Tachykinin NK2 Receptor Antagonists

Autor: Sandro Giuliani, Maria Altamura, Carlo Alberto Maggi, Antonio Guidi, Rose-Marie Catalioto, Stefania Meini, Alessandro Giolitti, Danilo Giannotti, Nicholas J. S. Harmat, Alessandro Lecci, Franco Pasqui, and Antonio Triolo, Rossano Nannicini, Manuela Tramontana, Valentina Fedi

Publikováno v: Journal of Medicinal Chemistry. 50:4793-4807

Starting from 1 (MEN14268), a selective tachykinin NK2 receptor antagonist with an interesting in vitro pharmacological profile, a family of numerous antagonists was obtained through an optimization process focused on iterated structural modification

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bb62c63baa13610c288dc04ab911ed8
https://doi.org/10.1021/jm070289w

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Insertion of 2-Carboxysuccinate and Tricarballylic Acid Fragments into Cyclic-Pseudopeptides: New Antagonists for the Human Tachykinin NK-2 Receptor

Autor: Sandro Giuliani, Marco Criscuoli, Enzo Perrotta, Carlo Alberto Maggi, Rossano Nannicini, Anna-Rita Renzetti, Nicholas J. S. Harmat, Riccardo Patacchini, Maria Altamura, Danilo Giannotti

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 12:693-696

A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-( d )-PheΨCH 2 NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72b9dfa9964747884d155ec03692e459
https://doi.org/10.1016/s0960-894x(01)00841-1

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2,6-Diketopiperazines from Amino Acids, from Solution-Phase to Solid-Phase Organic Synthesis

Autor: Teresa Barani, Danilo Giannotti, Carlo Alberto Maggi, Maria Altamura, Enzo Perrotta, Simona Bindi, Nicholas J. S. Harmat, Rossano Nannicini

Publikováno v: Journal of Combinatorial Chemistry. 3:453-460

A method to prepare 1,3-disubstituted 2,6-diketopiperazines (2,6-DKP) as useful heterocyclic library scaffolds in the search of new leads for drug discovery is described. The method can be used in solution-phase and solid-phase conditions. In the key

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::761f52d46ed01cea94ffd5356830d186
https://doi.org/10.1021/cc0000904

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Enantioselective syntheses of orthogonally protected tricarballylic acid esters

Autor: Danilo Giannotti, Maria Altamura, Enzo Perrotta, Rossano Nannicini, Nicholas J. S. Harmat, Silvia Mangani

Publikováno v: Tetrahedron Letters. 41:1261-1264

3( S ) and 3( R )-Benzyloxycarbonyl-pentanedioic acid mono- tert -butyl esters ( 6 ) were obtained as enantiopure orthogonally protected tricarballylic acid (TCA) esters. These were synthesised by alkylation of the sodium enolate derived from chiral

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ec90f2c317d15822a4192c457e61c36b
https://doi.org/10.1016/s0040-4039(99)02264-9

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4-Diazinyl- and 4-Pyridinylimidazoles: Potent Angiotensin II Antagonists. A Study of Their Activity and Computational Characterization

Autor: Anna Rita Renzetti, Fabrizio Bonaccorsi, Spartaco Mauro Colombani, C. Ghio, R. Giorgi, Nicholas J. S. Harmat, G. Alagona, Rocco Cirillo, Guido Cerbai, Alessandro Subissi

Publikováno v: Journal of Medicinal Chemistry. 38:2925-2937

A series of N-[biphenylyl(tetrazolyl)methyl]-2-butylimidazoles containing variously substituted diazine or pyridine moieties either as their free bases or N-oxide derivatives attached to the 4-position of the imidazole ring was synthesized and tested

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bef8ecdcce3f7d82cbfbe10ab43eeec
https://doi.org/10.1021/jm00015a015

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