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7-Azetidinylquinolones as Antibacterial Agents. 2. Synthesis and Biological Activity of 7-(2,3-Disubstituted-1-azetidinyl)-4-oxoquinoline- and -1,8-naphthyridine-3-carboxylic Acids. Properties and Structure-Activity Relationships of Quinolones with an Azetidine Moiety

Autor: Jordi Frigola, Calvet C, Redondo J, Antoni Torrens, Josep Mas, José A. Castrillo, Santiago García-Granda, David Vano, Berrocal Jm, Salgado L

Publikováno v: Journal of Medicinal Chemistry. 37:4195-4210

A series of 7-(2,3-disubstituted-1-azetidinyl)-1,4-dihydro-6-fluoro-4- oxoquinoline- and -1,8-naphthyridine-3-carboxylic acids, with varied substituents at the 1-, 5-, and 8-positions, was prepared to study the effects on potency and physicochemical

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2db26cffbc3346876db38bdd4fe85ef
https://doi.org/10.1021/jm00050a016

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A medicinal-chemistry-guided approach to selective and druglike sigma 1 ligands

Publikováno v: ChemMedChem. 1(1)

Based on a medicinal-chemistry-guided approach, three novel series of druglike cycloalkyl-annelated pyrazoles were synthesized and display high affinity (pKi>8) for the sigma1 receptor. Structure-affinity relationships were established, and the diffe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f200a1ba8122a9a10004c1b83f3077ec
https://pubmed.ncbi.nlm.nih.gov/16892345

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7-Azetidinylquinolones as antibacterial agents. 3. Synthesis, properties and structure-activity relationships of the stereoisomers containing a 7-(3-amino-2-methyl-1-azetidinyl) moiety

Autor: Edmundo Ortega, Jordi Frigola, David Vano, Santiago García-Granda, Angels Gomez-Gomar, Antoni Torrens

Publikováno v: Journal of medicinal chemistry. 38(7)

A series of stereochemically pure 7-(3-amino-2-methyl-1-azetidinyl)-1,4- dihydro-6-fluoro-4-oxoquinoline- and -1,8-naphthyridine-3-carboxylic acids, with varied substituents at the 1-, 5-, and 8-positions, was prepared to determine the effects of chi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dec1cd7948a27f7680509910ccf8ec5a
https://pubmed.ncbi.nlm.nih.gov/7707323

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