title: Molecular modulation of muscarinic antagonists. Synthesis and affinity profile of 2,2-diphenyl-2-ethylthio-acetic acid esters designed to probe the binding site cavity.
abstract: The synthesis and preliminary pharmacological profile of a new series of muscarinic antagonists, derived from previously studied 2,2-diphenyl-2-ethylthio-acetic acid esters, are reported. The parent molecules were decorated with linkers of different length, carrying an amino group to catch a putative anionic function outside the recognition site of the receptor. It was hoped that the interception of this function would give molecules with higher potency and selectivity. The attempt has not been successful, but a new series of compounds with a peculiar pharmacological profile has been identified.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. serena.scapecchi@unifi.it
authors.forename: Serena
authors.initials: S
authors.lastname: Scapecchi
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Martini
authors.forename: Cristina
authors.initials: C
authors.lastname: Bellucci
authors.forename: Michela
authors.initials: M
authors.lastname: Buccioni
authors.forename: Silvia
authors.initials: S
authors.lastname: Dei
authors.forename: Luca
authors.initials: L
authors.lastname: Guandalini
authors.forename: Dina
authors.initials: D
authors.lastname: Manetti
authors.forename: Cecilia
authors.initials: C
authors.lastname: Martelli
authors.forename: Gabriella
authors.initials: G
authors.lastname: Marucci
authors.forename: Rosanna
authors.initials: R
authors.lastname: Matucci
mesh_terms: D019342:Acetic Acid / Q000138:chemical synthesis* / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites / Q000502:physiology; D016466:CHO Cells; D006224:Cricetinae; D015195:Drug Design; D004952:Esters; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D008297:Male; D008968:Molecular Conformation; D018727:Muscarinic Antagonists / Q000138:chemical synthesis* / Q000378:metabolism*; D011817:Rabbits
chemical_list: D004952:Esters; D018727:Muscarinic Antagonists; D019342:Acetic Acid