New dibenzothiadiazepine derivatives with antidepressant activities.
A new series of 11-[(aminoalkyl)carbonyl] derivatives of 6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide (10-39) were synthesized and evaluated for potential antidepressant activity in the apomorphine-induced hypothermia (Apo 16) test. Effects on reserpine-induced hypothermia and toxicity for the most potent antagonists of Apo 16 hypothermia were also studied. Structure-activity relationships are reported. Anticholinergic effects were evaluated for compound 12, identified as the most potent and least toxic in this series, by assessing physostigmine lethality. Compound 12 was also subjected to X-ray analysis.
Giannotti
D
D
Dipartimento Ricerche Chimiche e Farmacologiche, A. Menarini Industrie Farmaceutiche Riunite S.r.l., Firenze, Italy.
Viti
G
G
Sbraci
P
P
Pestellini
V
V
Volterra
G
G
Borsini
F
F
Lecci
A
A
Meli
A
A
Dapporto
P
P
Paoli
P
P
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis*; D001058:Apomorphine / Q000494:pharmacology; D001831:Body Temperature / Q000187:drug effects; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D010830:Physostigmine / Q000633:toxicity; D012110:Reserpine / Q000494:pharmacology; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013841:Thiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014961:X-Ray Diffraction
D000928:Antidepressive Agents; D007202:Indicators and Reagents; D013841:Thiazepines; D012110:Reserpine; D010830:Physostigmine; D001058:Apomorphine