Synthesis and benzodiazepine receptor binding of some 4H-pyrimido[2,1-b]benzothiazol-4-ones

Article abstract of DOI:10.1016/0223-5234(92)90058-9

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.