Synthesis and CNS activities of pyridopyrazinone and pyridodiazepinone derivatives.
New tricyclic derivatives with cyclocondensed pyrido-pyrazine 7,10 and pyrido-diazepine 20a,20b skeletons were synthetized and biologically investigated. The compounds, preliminarily tested on explorative, muscle relaxing, antinociceptive, spontaneous motor activities and influence on the narcotic effect of Evipan, revealed interesting CNS depressant and analgesic activities. The pyrido[2,3-e]pyrrolo[1,2-a]pyrazine structure of 7 appeared the most promising for analgesic and neuroleptic activities. The above compounds were assayed also for their capacity to inhibit DNA synthesis in Ehrlich ascites tumor cells; 20a appeared to be able of inducing a significant inhibition.
Savelli
F
F
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Boido
A
A
Satta
M
M
Peana
A
A
Marzano
C
C
D000700:Analgesics / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002286:Carcinoma, Ehrlich Tumor / Q000378:metabolism; D002491:Central Nervous System Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004273:DNA, Neoplasm / Q000096:biosynthesis; D003975:Diazepam / Q000494:pharmacology; D005106:Exploratory Behavior / Q000187:drug effects; D006591:Hexobarbital / Q000037:antagonists & inhibitors / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000138:chemical synthesis / Q000494:pharmacology; D010147:Pain Measurement / Q000187:drug effects; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology
D000700:Analgesics; D000970:Antineoplastic Agents; D002491:Central Nervous System Agents; D004273:DNA, Neoplasm; D009125:Muscle Relaxants, Central; D011719:Pyrazines; D006591:Hexobarbital; D003975:Diazepam