Starting from a previously studied muscarinic ligand, characterized by a 1,3-oxathiolane nucleus, a new series of muscarinic antagonists were designed by increasing the stereochemical complexity of the molecules. A small library of enantiomeric and diastereomeric 2,2-diphenyl- and 2-cyclohexyl- 2-phenyl substituted compounds was thus obtained. All the tested compounds show a high affinity toward cloned human muscarinic hm1-hm5 receptors expressed in CHO cells and a good antagonistic activity on functional assays, with a modest selectivity on rabbit vas deferens
SYNTHESIS, AFFINITY PROFILE AND FUNCTIONAL ACTIVITY OF MUSCARINIC ANTAGONISTS WITH A 1-METHYL-2-(2,2-ALKYLARYL-1,3-OXATHIOLAN-5-YL)PYRROLIDINE STRUCTURE / Dei, Silvia; Bellucci, Cristina; Buccioni, M.; Ferraroni, Marta; Guandalini, Luca; Manetti, Dina; Martini, Elisabetta; Marucci, G.; Matucci, Rosanna; Nesi, Marta; Romanelli, MARIA NOVELLA; Scapecchi, Serena; Teodori, Elisabetta. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 50:(2007), pp. 1409-1413. [10.1021/jm061374r]
SYNTHESIS, AFFINITY PROFILE AND FUNCTIONAL ACTIVITY OF MUSCARINIC ANTAGONISTS WITH A 1-METHYL-2-(2,2-ALKYLARYL-1,3-OXATHIOLAN-5-YL)PYRROLIDINE STRUCTURE
DEI, SILVIA;BELLUCCI, CRISTINA;FERRARONI, MARTA;GUANDALINI, LUCA;MANETTI, DINA;MARTINI, ELISABETTA;MATUCCI, ROSANNA;NESI, MARTA;ROMANELLI, MARIA NOVELLA;SCAPECCHI, SERENA;TEODORI, ELISABETTA
2007
Abstract
Starting from a previously studied muscarinic ligand, characterized by a 1,3-oxathiolane nucleus, a new series of muscarinic antagonists were designed by increasing the stereochemical complexity of the molecules. A small library of enantiomeric and diastereomeric 2,2-diphenyl- and 2-cyclohexyl- 2-phenyl substituted compounds was thus obtained. All the tested compounds show a high affinity toward cloned human muscarinic hm1-hm5 receptors expressed in CHO cells and a good antagonistic activity on functional assays, with a modest selectivity on rabbit vas deferensFile | Dimensione | Formato | |
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