European Journal of Medicinal Chemistry p. 39 - 44 (1992)
Update date:2022-08-29
Topics:
Trapani
Franco
Latrofa
Genchi
Liso
Synthesis and ability to displace [3H]diazepam binding from rat brain membranes of the 3-(alkoxycarbonyl)-4H-pyrimido[2,1-b]benzothiazol-4-ones 3a-p and related compounds 10-12 are described. It has been found that some compounds bind to the benzodiazepine receptor (BZR) with potency greater than chlordiazepoxide. From a structure-affinity point of view the substitution at 6-position of pyrimido[2,1-b]benzothiazole nucleus was found conductive to higher affinity. In vitro data (GABA ratio) lend support to the fact that the most active compounds 3j, 1 might possess agonist properties at BZR.
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