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举例 :可输入Filippa Pettersson 或者 Cancer Res. 75(6) , 1102-12, (2015) 或者10.1002/anie.201600521

Heteroarenobenzodiazepines. 3. 4-Piperazinyl-10H-thieno [2, 3-b][1, 5] benzodiazepines as potential neuroleptics

JK Chakrabarti, L Horsman, TM Hotten…

文献索引：Chakrabarti, Jiban K.; Horsman, Linda; Hotten, Terrence M.; Pullar, Ian A.; Tupper, David E. Journal of Medicinal Chemistry, 1980 , vol. 23, # 8 p. 878 - 884

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被引用次数: 85

摘要

A series of 4-substituted lOH-thieno [2,341 [1, 5] benzodiazepines has been synthesized. These compounds have been assessed for their ability to block a conditioned avoidance response (CAR) and to produce catalepsy in rats and have been compared with several typical and atypical neuroleptics. The compounds which inhibit CAR at doses which produce no catalepsy we believed to cause less extrapyramidal side effects in the clinic. A number ...

ethyl 2-(4-fluoro-2-nitroanilino)-4-methylthiophene-3-carboxylate结构式

ethyl 2-(4-fluo...

~%

7-Fluoro-3-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno(2,3-b)(1,5)ben zodiazepine结构式

7-Fluoro-3-meth...

2-ethyl-7-nitro-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-7-nitro...

N-甲基哌嗪结构式

~10%

2-Ethyl-4-(4-methyl-1-piperazinyl)-7-nitro-10H-thieno(2,3-b)(1,5)benzo diazepine结构式

2-Ethyl-4-(4-me...

N-甲基哌嗪结构式

7-fluoro-2-methyl-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

7-fluoro-2-meth...

~35%

氟甲氮平结构式

N-甲基哌嗪结构式

7-fluoro-2-isopropyl-5,10-dihydro-4H-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

7-fluoro-2-isop...

~55%

7-fluoro-4-(4-methylpiperazin-1-yl)-2-propan-2-yl-5H-thieno[3,2-c][1,5]benzodiazepine结构式

7-fluoro-4-(4-m...

2-ethyl-4-piperazin-1-yl-5H-thieno[3,2-c][1,5]benzodiazepine结构式

2-ethyl-4-piper...

溴代丙烷结构式

~20%

2-ethyl-4-(4-propylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine结构式

2-ethyl-4-(4-pr...

ethyl 4-(2-ethyl-5H-thieno[3,2-c][1,5]benzodiazepin-4-yl)piperazine-1-carboxylate结构式

ethyl 4-(2-ethy...

~%

2-ethyl-4-(4-propylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine结构式

2-ethyl-4-(4-pr...

2-ethyl-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-5,10-di...

~%

2-ethyl-4-(4-propylpiperazin-1-yl)-5H-thieno[3,2-c][1,5]benzodiazepine结构式

2-ethyl-4-(4-pr...

N-甲基哌嗪结构式

2-acetyl-4,10-dihydro-benzo[e]thieno[3,2-b][1,4]diazepin-5-one结构式

2-acetyl-4,10-d...

~6%

1-[5-(4-methylpiperazin-1-yl)-4H-thieno[2,3-b][1,4]benzodiazepin-2-yl]ethanone结构式

1-[5-(4-methylp...

2-ethyl-7-fluoro-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-7-fluor...

~%

2-ethyl-7-fluoro-N-[2-(4-phenylpiperazin-1-yl)ethyl]-5H-thieno[3,2-c][1,5]benzodiazepin-4-amine结构式

2-ethyl-7-fluor...

2-(4-苯基-哌嗪-1-基)-乙胺结构式

2-(4-苯基-哌嗪-1-基)-乙胺

2-ethyl-7-fluoro-5,10-dihydro-4H-thieno[2,3-b][1,5]benzodiazepine-4-thione结构式

2-ethyl-7-fluor...

~%

2-ethyl-7-fluoro-N-[2-(4-phenylpiperazin-1-yl)ethyl]-5H-thieno[3,2-c][1,5]benzodiazepin-4-amine结构式

2-ethyl-7-fluor...

N-甲基哌嗪结构式

2-ethyl-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-5,10-di...

~63%

2-乙基-4-<4-甲基-1-哌嗪基>-10H-噻吩并<2,3-B><1,5>苯并二氮卓结构式

2-乙基-4-<4-甲基-1-...

2-ethyl-7-fluoro-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-7-fluor...

~%

2-ethyl-7-fluoro-N-[3-(4-methylpiperazin-1-yl)propyl]-5H-thieno[3,2-c][1,5]benzodiazepin-4-amine结构式

2-ethyl-7-fluor...

1-(3-氨丙基)-4-甲基哌嗪结构式

1-(3-氨丙基)-4-甲基哌嗪

2-ethyl-7-fluoro-5,10-dihydro-4H-thieno[2,3-b][1,5]benzodiazepine-4-thione结构式

2-ethyl-7-fluor...

~%

2-ethyl-7-fluoro-N-[3-(4-methylpiperazin-1-yl)propyl]-5H-thieno[3,2-c][1,5]benzodiazepin-4-amine结构式

2-ethyl-7-fluor...

2-ethyl-7-fluoro-4-piperazin-1-yl-5H-thieno[3,2-c][1,5]benzodiazepine结构式

2-ethyl-7-fluor...

4-氯溴苄结构式

~59%

4-[4-[(4-chlorophenyl)methyl]piperazin-1-yl]-2-ethyl-7-fluoro-5H-thieno[3,2-c][1,5]benzodiazepine结构式

4-[4-[(4-chloro...

2-ethyl-7-fluoro-4-[4-(carboethoxy)-1-piperazinyl]-10H-thieno[2,3-b][1,5]benzodiazepine结构式

2-ethyl-7-fluor...

~%

4-[4-[(4-chlorophenyl)methyl]piperazin-1-yl]-2-ethyl-7-fluoro-5H-thieno[3,2-c][1,5]benzodiazepine结构式

4-[4-[(4-chloro...

2-ethyl-7-fluoro-5,10-dihydro-benzo[b]thieno[2,3-e][1,4]diazepin-4-one结构式

2-ethyl-7-fluor...

~%

4-[4-[(4-chlorophenyl)methyl]piperazin-1-yl]-2-ethyl-7-fluoro-5H-thieno[3,2-c][1,5]benzodiazepine结构式

4-[4-[(4-chloro...