The synthesis and pharmacological activity of two new derivatives of benzazocine.

Two new derivatives of benzazocine of anticipated analgesic action were synthesized. Pharmacological investigations were carried out to confirm their analgesic activity, affinity to the opiate receptor and potential antagonistic properties.

Synthesis and preliminary pharmacological screening of 4-methylamino-2-phenylquinoline-3-carboxamides.

Eight new 4-methylamino-2-phenylquinoline-3-carboxamides were obtained. Three of them were screened pharmacologically and all turned out to be antiinflammatory, analgesic and sedative compounds. Their properties were compared to those of indomethacin and pethidine.

Analgesic and antiinflammatory properties of the pirolo-[3,4-e] [1,4]-diazepine derivatives.

Pirolo [3,4-e] [1,4]-diazepine derivatives: 5-(2'-naphtyl) (7-phenyl-) 2, 3, 6, 8-tetrahydro)-pirolo-[3,4-e] [1,4]-diazepine-6-thiox-8-(1H,7H)-one (PD) and 5-(2'-naphtyl) 7-p-chlorophenyl-(2, 3, 6, 8-tetrahydro)-pirolo-[3,4-e] [1,4]-diazepine-6-thiox-8-(1H, 7H)-one (PDC1) show distinct analgesic properties, but no marked antiinflammatory activity in vivo. In addition these compounds inhibit rat blood platelet aggregation in vivo, and produce contractions of the rat's pregnant uterus.

Analgesic and anti-inflammatory properties of 4-propionyl-4-(4-chlorophenyl)-1-(3-dimethylaminopropyl)-piperidine dihydrochloride.

4-propionyl-4-(4-chlorophenyl)-1-(3-dimethylaminopropyl)-piperidine dihydro-chloride (S8) showed in the hot plate test a marked analgesic activity with a better therapeutic index than that of pethidine. S8 possesses also anti-inflammatory (in short and long-term tests in vivo) as well as spasmolytic properties.