[Compounds with psychotropic activity. VIII. Synthesis and sedative activity of various 9-substituted derivatives of 5-phenylpyrrolo[2,1-d][1,5] benzothiazepine and cis-4,5-dihydro-4-hydroxy-5-phenylpyrrolo[2,1-d][1,5]benzothiazepine].
Syntheses of 9-chloro-, 9-trifluoromethyl- and 9-methoxy-5- phenylpyrrolo [2,1-d] [1,5] benzothiazepine [II a-c] and of cis-9-chloro- and cis-9-trifluoromethyl-4,5-dihydro-4-hydroxy-5- phenylpyrrolo [2,1-d] [1,5] benzothiazepine with the respective acetyl derivatives (III a-d), according to previously restated routes, are described. The sedative activity was tested against the anti-amphetamine activity in the rat. The 1-[5-trifluoromethyl-2-(alpha- hydroxycarbonylbenzyl ) thiophenyl + ++]-pyrrole ( NF34 ) and the pyrrolo [2,1-d] [1,5] benzothiazepine -5-carboxamide ( NF44 ) showed sedative activity similar to that of diazepam.
D000661:Amphetamine / Q000037:antagonists & inhibitors; D000818:Animals; D005260:Female; D006993:Hypnotics and Sedatives / Q000138:chemical synthesis*; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013841:Thiazepines / Q000138:chemical synthesis* / Q000494:pharmacology
D006993:Hypnotics and Sedatives; D013841:Thiazepines; D000661:Amphetamine
Ricerche su composti ad attività psicotropa. Nota VIII - Sintesi ed attività sedativa di alcuni derivati 9-sostituiti della 5-fenilpirrolo [2,1-d] [1,5]benzotiazepina e della cis-4,5-diidro-4-idrossi-5-fenilpirrolo [2,1-d] [1,5]benzotiazepina.