Abstract
Summary A number of new pyrrolobenzothiazepine derivatives and a pyrrolobenzothiazocine derivative have been synthesized and evaluated for their affinity towards the ‘peripheral-type’ benzodiazepine receptor (PBR). The new compounds were tested in rat cortex, a tissue expressing a high density of mitochondrial PBR. Some of the pyrrolobenzothiazepines exhibited IC50 values in the low nanomolar range as measured by the displacement of [3H]PK 11195 binding. Compound 4i was found to be the most potent ligand for this receptor in the pyrrolobenzothiazepine subgroup with an IC50 practically identical to that determined for PK 11195. Structure—affinity relationships (SARs) have been developed to elucidate the topology of the PBR binding site.
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