Bioorganic & Medicinal Chemistry Letters

Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands

M Kassiou, RW Read, X Shi

Index: Kassiou, Michael; Read, Roger W.; Shi, Xue-Qin Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 7 p. 799 - 804

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Citation Number: 2

Abstract

Syntheses of four novel amide analogues of the muscarinic M2 receptors antagonists, DIBA and BIBN 140, are described from a common intermediate. Pharmacological evaluation through in vitro assays reveals high muscarinic receptor affinity in each of the compounds, but variable subtype selectivity, primarily M2 but in one case M3.