NEW DIBENZOTHIADIAZEPINE DERIVATIVES WITH ANTIDEPRESSANT ACTIVITIES

被引:31
作者
GIANNOTTI, D [1 ]
VITI, G [1 ]
SBRACI, P [1 ]
PESTELLINI, V [1 ]
VOLTERRA, G [1 ]
BORSINI, F [1 ]
LECCI, A [1 ]
MELI, A [1 ]
DAPPORTO, P [1 ]
PAOLI, P [1 ]
机构
[1] UNIV FLORENCE,DIPARTIMENTO ENERGET,I-50139 FLORENCE,ITALY
关键词
D O I
10.1021/jm00108a018
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1356 / 1362
页数:7
相关论文
共 29 条
[1]   MOLECULAR-CONFORMATION AND BIOLOGICAL-ACTIVITY OF CENTRAL NERVOUS-SYSTEM ACTIVE-DRUGS [J].
ANDREWS, PR ;
LLOYD, EJ .
MEDICINAL RESEARCH REVIEWS, 1982, 2 (04) :355-393
[2]  
BALDESSARINI RJ, 1985, PHARMACOL BASIS THER, pCH19
[3]   HYPOTENSIVE 1,2,4-BENZOTHIADIAZINES [J].
BIERBAUM, BA ;
TRAVERSO, JJ ;
WHITEHEAD, CW .
JOURNAL OF MEDICINAL CHEMISTRY, 1963, 6 (03) :272-&
[4]  
BLACKWELL B, 1986, Drugs of Today, V22, P611
[5]  
BORSINI F, 1988, ITAL PATENT, P9466
[6]  
BORSINI F, IN PRESS ARZNEIM FOR
[7]  
BOURIN M, 1983, ARZNEIMITTELFORSCH, V33-2, P1173
[8]  
de Paulis T, 1978, Mol Pharmacol, V14, P596
[9]  
DEFRANCE R, 1988, CLIN NEUROPHARMAC S2, V11, P74
[10]   On phenylation of primary aromatic amines. [J].
Goldberg, I .
BERICHTE DER DEUTSCHEN CHEMISCHEN GESELLSCHAFT, 1907, 40 :4541-4546