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 deferens
2007
50
1409
1413
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
File in questo prodotto:
File Dimensione Formato  
jmc_antag_07.pdf

Accesso chiuso

Tipologia: Altro
Licenza: Tutti i diritti riservati
Dimensione 105.32 kB
Formato Adobe PDF
105.32 kB Adobe PDF   Richiedi una copia

I documenti in FLORE sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/26824
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 11
  • ???jsp.display-item.citation.isi??? 11
social impact