[Research on a compound with psychotropic activity. V - a new derivative of pyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide: synthesis and sedative activity]. / Ricerche su composti ad attività psicotropa. Nota V - nuovi derivati del pirrolo[2,1-d][1,5]benzotiazepin-6,6-diossido: sintesi ed attività sedativa.

The following compounds have been synthesized according to a previously tested route, of the 9-chloro-, 9-trifluoromethyl- and 9-methoxy-5-phenylpyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (II a-c), 9-chloro- and 9-trifluoromethyl-5-p-nitrophenylpyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (II d, e), 5-(4-pyridyl)pyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (III) and 5-(3-pyridyl)pyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (IVa) with the 9-chloro- and 9-trifluoromethyl- derivatives (IV b, c) are reported. The sedative action in the rat was tested against the motor activity induced by amphetamine. The 9-chloro-5(3-pyridyl)pyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide was particularly active and showed sedative action superior to that of diazepam. Marked sedative activity was observed with 9-methoxy-5-phenylpyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (NF19) and 9-chloro-5-p-nitrophenylpyrrolo[2,1-d][1,5]benzothiazepin-6,6-dioxide (NF20).