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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

Identification of 2-arylbenzimidazoles as potent human histamine H 4 receptor ligands

A Lee-Dutra, KL Arienti, DJ Buzard, MD Hack…

文献索引：Lee-Dutra, Alice; Arienti, Kristen L.; Buzard, Daniel J.; Hack, Michael D.; Khatuya, Haripada; Desai, Pragnya J.; Nguyen, Steven; Thurmond, Robin L.; Karlsson, Lars; Edwards, James P.; Breitenbucher, J. Guy Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 23 p. 6043 - 6048

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被引用次数: 53

摘要

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H4 receptor. Structure–activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H4 receptor.

4-(4-羟基丁-1-炔-1-基)苯甲醛结构式

4-(4-羟基丁-1-炔-1-基)苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)but-1-enyl]benzaldehyde结构式

4-[4-(4-methylp...

对溴苯甲醛结构式

对溴苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)but-1-enyl]benzaldehyde结构式

4-[4-(4-methylp...

N-甲基哌嗪结构式

~%

4-[4-(4-methylpiperazin-1-yl)but-1-enyl]benzaldehyde结构式

4-[4-(4-methylp...

4-(4-formylphenyl)but-3-ynyl methanesulfonate结构式

4-(4-formylphen...

~%

4-[4-(4-methylpiperazin-1-yl)but-1-enyl]benzaldehyde结构式

4-[4-(4-methylp...

4-[4-(4-methylpiperazin-1-yl)but-1-ynyl]benzaldehyde结构式

4-[4-(4-methylp...

~%

4-[4-(4-methylpiperazin-1-yl)but-1-enyl]benzaldehyde结构式

4-[4-(4-methylp...

未登录结构式

4-羟基-3-碘苯甲腈结构式

4-羟基-3-碘苯甲腈

3-丁炔-1-醇结构式

~99%

2-(2-hydroxyethyl)-1-benzofuran-5-carbonitrile结构式

2-(2-hydroxyeth...

4-羟基苯甲腈结构式

4-羟基苯甲腈

~%

2-(2-hydroxyethyl)-1-benzofuran-5-carbonitrile结构式

2-(2-hydroxyeth...

N-甲基哌嗪结构式

1-(3-formylphenoxy)-3-chloropropane结构式

1-(3-formylphen...

~%

3-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3-[3-(4-methylp...

间羟基苯甲醛结构式

间羟基苯甲醛

~%

3-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3-[3-(4-methylp...

2-(2-hydroxyethyl)-1-benzofuran-5-carbonitrile结构式

2-(2-hydroxyeth...

甲基磺酰氯结构式

甲基磺酰氯

~99%

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

4-羟基-3-碘苯甲腈结构式

4-羟基-3-碘苯甲腈

~%

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

4-羟基苯甲腈结构式

4-羟基苯甲腈

~%

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

N-甲基哌嗪结构式

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

~46%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbonitrile结构式

2-[2-(4-methylp...

2-(2-hydroxyethyl)-1-benzofuran-5-carbonitrile结构式

2-(2-hydroxyeth...

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbonitrile结构式

2-[2-(4-methylp...

4-羟基-3-碘苯甲腈结构式

4-羟基-3-碘苯甲腈

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbonitrile结构式

2-[2-(4-methylp...

4-羟基苯甲腈结构式

4-羟基苯甲腈

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbonitrile结构式

2-[2-(4-methylp...

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbonitrile结构式

2-[2-(4-methylp...

~57%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

N-甲基哌嗪结构式

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

~46%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

2-(2-hydroxyethyl)-1-benzofuran-5-carbonitrile结构式

2-(2-hydroxyeth...

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

4-羟基-3-碘苯甲腈结构式

4-羟基-3-碘苯甲腈

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

4-羟基苯甲腈结构式

4-羟基苯甲腈

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

2-(5-cyano-1-benzofuran-2-yl)ethyl methanesulfonate结构式

2-(5-cyano-1-be...

~%

2-[2-(4-methylpiperazin-1-yl)ethyl]-1-benzofuran-5-carbaldehyde结构式

2-[2-(4-methylp...

N-甲基哌嗪结构式

4-(4-Chlorobutoxy)benzaldehyde结构式

4-(4-Chlorobuto...

~%

4-[4-(4-methylpiperazin-1-yl)butoxy]benzaldehyde结构式

4-[4-(4-methylp...

4-羟基苯甲醛; 对羟基苯甲醛结构式

4-羟基苯甲醛; 对羟基苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)butoxy]benzaldehyde结构式

4-[4-(4-methylp...

对溴苯甲醛结构式

对溴苯甲醛

3-丁炔-1-醇结构式

~99%

4-(4-羟基丁-1-炔-1-基)苯甲醛结构式

4-(4-羟基丁-1-炔-1-基)苯甲醛

1-Boc-4-(3-羟基苯基)哌嗪结构式

1-Boc-4-(3-羟基苯基)哌嗪

~%

4-[3-(4-methylpiperazin-1-yl)phenoxy]benzaldehyde结构式

4-[3-(4-methylp...

间羟基苯基哌嗪结构式

间羟基苯基哌嗪

~%

4-[3-(4-methylpiperazin-1-yl)phenoxy]benzaldehyde结构式

4-[3-(4-methylp...

4-(4-羟基丁-1-炔-1-基)苯甲醛结构式

4-(4-羟基丁-1-炔-1-基)苯甲醛

甲基磺酰氯结构式

甲基磺酰氯

~99%

4-(4-formylphenyl)but-3-ynyl methanesulfonate结构式

4-(4-formylphen...

对溴苯甲醛结构式

对溴苯甲醛

~%

4-(4-formylphenyl)but-3-ynyl methanesulfonate结构式

4-(4-formylphen...

3-氯-4-羟基苯甲醛结构式

3-氯-4-羟基苯甲醛

~%

3-chloro-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3-chloro-4-[3-(...

N-甲基哌嗪结构式

未登录结构式

~%

2-methoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

2-methoxy-4-[3-...

4-羟基-2-甲氧基苯甲醛结构式

4-羟基-2-甲氧基苯甲醛

~%

2-methoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

2-methoxy-4-[3-...

N-甲基哌嗪结构式

4-(4-formylphenyl)but-3-ynyl methanesulfonate结构式

4-(4-formylphen...

~41%

4-[4-(4-methylpiperazin-1-yl)but-1-ynyl]benzaldehyde结构式

4-[4-(4-methylp...

4-(4-羟基丁-1-炔-1-基)苯甲醛结构式

4-(4-羟基丁-1-炔-1-基)苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)but-1-ynyl]benzaldehyde结构式

4-[4-(4-methylp...

对溴苯甲醛结构式

对溴苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)but-1-ynyl]benzaldehyde结构式

4-[4-(4-methylp...

2-氯-4-羟基苯甲醛结构式

2-氯-4-羟基苯甲醛

~%

2-chloro-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

2-chloro-4-[3-(...

3-羟基-4-甲基苯甲醛结构式

3-羟基-4-甲基苯甲醛

~%

4-methyl-3-[4-(4-methylpiperazin-1-yl)butoxy]benzaldehyde结构式

4-methyl-3-[4-(...

N-甲基哌嗪结构式

3-methoxy-4-(3-chloropropoxy) benzaldehyde结构式

3-methoxy-4-(3-...

~%

3-methoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3-methoxy-4-[3-...

香草醛结构式

~%

3-methoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3-methoxy-4-[3-...

N-甲基哌嗪结构式

未登录结构式

~%

3,5-dimethyl-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3,5-dimethyl-4-...

3,5-二甲基-4-羟基苯甲醛结构式

3,5-二甲基-4-羟基苯甲醛

~%

3,5-dimethyl-4-[3-(4-methylpiperazin-1-yl)propoxy]benzaldehyde结构式

3,5-dimethyl-4-...

4-[4-(4-methylpiperazin-1-yl)but-1-ynyl]benzaldehyde结构式

4-[4-(4-methylp...

~80%

4-[4-(4-methylpiperazin-1-yl)butyl]benzaldehyde结构式

4-[4-(4-methylp...

N-甲基哌嗪结构式

~%

4-[4-(4-methylpiperazin-1-yl)butyl]benzaldehyde结构式

4-[4-(4-methylp...

4-(4-羟基丁-1-炔-1-基)苯甲醛结构式

4-(4-羟基丁-1-炔-1-基)苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)butyl]benzaldehyde结构式

4-[4-(4-methylp...

4-(4-formylphenyl)but-3-ynyl methanesulfonate结构式

4-(4-formylphen...

~%

4-[4-(4-methylpiperazin-1-yl)butyl]benzaldehyde结构式

4-[4-(4-methylp...

对溴苯甲醛结构式

对溴苯甲醛

~%

4-[4-(4-methylpiperazin-1-yl)butyl]benzaldehyde结构式

4-[4-(4-methylp...