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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

Synthesis of 2-(2, 3-dihydro-2-oxo-1, 3, 4-oxadiazol-5-yl) benzo heterocycles. A novel series of orally active antiallergic agents

…, RE Brown, B Loev, K Bailey, H Jones…

文献索引：Musser, John H.; Brown, Richard E.; Loev, Bernard; Bailey, Kevin; Jones, Howard; et al. Journal of Medicinal Chemistry, 1984 , vol. 27, # 2 p. 121 - 125

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被引用次数: 66

摘要

A series of new 2-(2, 3-dihydro-2-oxo-1, 3, 4-oxadiazol-5-y1) benzo heterocycles has been prepared. These compounds were tested as inhibitors of antigen-induced release of histamine (AIR) in vitro from rat peritoneal mast cells (RMC) and as inhibitors of IgE- mediated rat passive cutaneous anaphylaxis in the rat (PCA). Most of this new class of antiallergic agents showed good activity in the RMC assay. The most potent compound, 3- ...

ethyl 2-(5-chlorobenzo[d]oxazole-2-carbonyl)hydrazine-1-carboxylate结构式

ethyl 2-(5-chlo...

~%

5-(5-chloro-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(5-chloro-1,3...

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ethyl 2-(6-methylbenzo[d]oxazole-2-carbonyl)hydrazine-1-carboxylate结构式

ethyl 2-(6-meth...

~%

5-(6-methyl-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(6-methyl-1,3...

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3-chloro-7-methyl-1,4-benzoxazin-2-one结构式

3-chloro-7-meth...

~%

5-(6-methyl-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(6-methyl-1,3...

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ethyl 2-(4-methylbenzo[d]oxazole-2-carbonyl)hydrazine-1-carboxylate结构式

ethyl 2-(4-meth...

~%

5-(4-methyl-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(4-methyl-1,3...

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3-chloro-5-methyl-1,4-benzoxazin-2-one结构式

3-chloro-5-meth...

~%

5-(4-methyl-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(4-methyl-1,3...

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methyl 1,5-dimethylbenzimidazole-2-carboxylate结构式

methyl 1,5-dime...

~%

1,5-dimethylbenzimidazole-2-carbohydrazide结构式

1,5-dimethylben...

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methyl 3-methyl-1H-indene-2-carboxylate结构式

methyl 3-methyl...

~%

3-methyl-1H-indene-2-carbohydrazide结构式

3-methyl-1H-ind...

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5-甲基苯并[D]噁唑-2-甲酸甲酯结构式

5-甲基苯并[D]噁唑-2-甲酸甲酯

~%

5-(5-methyl-1,3-benzoxazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(5-methyl-1,3...

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乙酸酐结构式

2-(2,3-dihydro-1,3,4-oxadiazol-5-yl)benzoxazole结构式

2-(2,3-dihydro-...

~62%

3-acetyl-5-(1,3-benzoxazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1,3...

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3-CHLORO-2H-BENZO[B][1,4]OXAZIN-2-ONE结构式

3-CHLORO-2H-BEN...

~%

3-acetyl-5-(1,3-benzoxazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1,3...

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ethyl 3-(2-benzoxazolyl)hydrazinecarboxylate结构式

ethyl 3-(2-benz...

~%

3-acetyl-5-(1,3-benzoxazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1,3...

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苯并[d]噁唑-2-羧酸甲酯结构式

苯并[d]噁唑-2-羧酸甲酯

~%

3-acetyl-5-(1,3-benzoxazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1,3...

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3-CHLORO-2H-BENZO[B][1,4]OXAZIN-2-ONE结构式

3-CHLORO-2H-BEN...

~%

5-(1,3-benzoxazol-2-yl)-3-methyl-1,3,4-oxadiazol-2-one结构式

5-(1,3-benzoxaz...

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ethyl 3-(2-benzoxazolyl)hydrazinecarboxylate结构式

ethyl 3-(2-benz...

~%

5-(1,3-benzoxazol-2-yl)-3-methyl-1,3,4-oxadiazol-2-one结构式

5-(1,3-benzoxaz...

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苯并[d]噁唑-2-羧酸甲酯结构式

苯并[d]噁唑-2-羧酸甲酯

~%

5-(1,3-benzoxazol-2-yl)-3-methyl-1,3,4-oxadiazol-2-one结构式

5-(1,3-benzoxaz...

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2-(2,3-dihydro-1,3,4-oxadiazol-5-yl)benzoxazole结构式

2-(2,3-dihydro-...

~%

5-(1,3-benzoxazol-2-yl)-3-methyl-1,3,4-oxadiazol-2-one结构式

5-(1,3-benzoxaz...

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1-methyl-2-(trichloromethyl)benzimidazole结构式

1-methyl-2-(tri...

~%

3-acetyl-5-(1-methylbenzimidazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1-m...

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乙酸酐结构式

ethyl 3-(1-methyl-2-benzimidazolyl)hydrazinecarboxylate结构式

ethyl 3-(1-meth...

~%

3-acetyl-5-(1-methylbenzimidazol-2-yl)-1,3,4-oxadiazol-2-one结构式

3-acetyl-5-(1-m...

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1-甲基-1H-苯并咪唑-2-羧酸甲酯结构式

1-甲基-1H-苯并咪唑-2-羧酸甲酯

~91%

(9ci)-1-甲基-1H-苯并咪唑-2-羧酸肼结构式

(9ci)-1-甲基-1H-苯...

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methyl 1,5-dimethylbenzimidazole-2-carboxylate结构式

methyl 1,5-dime...

~%

5-(1,5-dimethylbenzimidazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(1,5-dimethyl...

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光气结构式

1,5-dimethylbenzimidazole-2-carbohydrazide结构式

1,5-dimethylben...

~%

5-(1,5-dimethylbenzimidazol-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(1,5-dimethyl...

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methyl 3-methyl-1H-indene-2-carboxylate结构式

methyl 3-methyl...

~%

5-(3-methyl-1H-inden-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(3-methyl-1H-...

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光气结构式

3-methyl-1H-indene-2-carbohydrazide结构式

3-methyl-1H-ind...

~%

5-(3-methyl-1H-inden-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(3-methyl-1H-...

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1-methyl-2-(trichloromethyl)benzimidazole结构式

1-methyl-2-(tri...

~%

(9ci)-1-甲基-1H-苯并咪唑-2-羧酸肼结构式

(9ci)-1-甲基-1H-苯...

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ethyl 3-(1-methyl-2-benzimidazolyl)hydrazinecarboxylate结构式

ethyl 3-(1-meth...

~85%

5-(1-benzofuran-2-yl)-3H-1,3,4-oxadiazol-2-one结构式

5-(1-benzofuran...

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甲醇结构式

1-methyl-2-(trichloromethyl)benzimidazole结构式

1-methyl-2-(tri...

~60%

1-甲基-1H-苯并咪唑-2-羧酸甲酯结构式

1-甲基-1H-苯并咪唑-2-羧酸甲酯

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1-苯并呋喃-2-羰酰氯结构式

1-苯并呋喃-2-羰酰氯

肼基甲酸乙酯结构式

肼基甲酸乙酯

~58%

ethyl N-(1-benzofuran-2-carbonylamino)carbamate结构式

ethyl N-(1-benz...

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