Synthesis, Biological Activity, and SARs of Pyrrolobenzoxazepine Derivatives, a New Class of Specific “Peripheral-Type” Benzodiazepine Receptor Ligands 1

…, E Novellino, DC Williams, DM Zisterer…

Index: Campiani, Giuseppe; Nacci, Vito; Fiorini, Isabella; De Filippis, Maria P.; Garofalo, Antonio; Ciani, Silvia M.; Greco, Giovanni; Novellino, Ettore; Williams, D. Clive; Zisterer, Daniela M.; Woods, Margaret J.; Mihai, Camelia; Manzoni, Cristina; Mennini, Tiziana Journal of Medicinal Chemistry, 1996 , vol. 39, # 18 p. 3435 - 3450

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Citation Number: 87

Abstract

The “peripheral-type” benzodiazepine receptor (PBR) has been reported to play a role in many biological processes. We have synthesized and tested a novel series of PBR ligands based on a pyrrolobenzoxazepine skeleton, in order to provide new receptor ligands. Several of these new compounds proved to be high affinity and selective ligands for PBR, and benzoxazepines 17f and 17j were found to be the most potent ligands for this receptor ...