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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 and anti-HIV activity of 1, 3, 4, 5-tetrahydro-2H-1, 4-benzodiazepin-2-one (TBO) derivatives. truncated 4, 5, 6, 7-tetrahydro-5-methylimidazo [4, 5, 1-jk][1, 4] …

…, H Cullis, F De Knaep, R Pauwels, K Andries…

文献索引：Breslin, Henry J.; Kukla, Michael J.; Kromis, Teresa; Cullis, Heather; De Knaep, Fons; Pauwels, Rudi; Andries, Koen; De Clercq, Erik; Janssen, Marcel A.C.; Janssen, Paul A.J. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 11 p. 2427 - 2436

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被引用次数: 33

摘要

4, 5, 6, 7-Tetrahydro-5-methylimidazo [4, 5, 1-jk][1, 4] benzodiazepin-2 (1H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication, as reported in detail in our prior publications. Since our earlier reports, we have modified the TIBO structures 1 by removing the 5-membered ring of 1, generating 1, 3, 4, 5-tetrahydro-2H-1, 4-benzodiazepin-2-ones (TBO), 4, a bicyclic series of compounds. Although compounds 4 possess modest activity ...

1-溴-3-甲基-2-丁烯结构式

1-溴-3-甲基-2-丁烯

3-methyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

3-methyl-1,3,4,...

~42%

3-methyl-4-(3-methylbut-2-enyl)-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

3-methyl-4-(3-m...

5-CHLORO-2-NITROBENZYLAMINE结构式

5-CHLORO-2-NITR...

~%

7-chloro-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-1,3,4,...

ethyl N-[(5-chloro-2-nitrophenyl)methyl]glycine结构式

ethyl N-[(5-chl...

~%

7-chloro-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-1,3,4,...

ethyl N-[(2-amino-5-chlorophenyl)methyl]glycine结构式

ethyl N-[(2-ami...

~19%

7-chloro-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-1,3,4,...

(+/-)-methyl 2-[[(2-amino-5-chlorophenyl)methyl]amino]-3-methylbutanoate结构式

(+/-)-methyl 2-...

~63%

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

5-氯-2-硝基苄醇结构式

5-氯-2-硝基苄醇

~%

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

DL-缬氨酸甲酯盐酸盐结构式

DL-缬氨酸甲酯盐酸盐

~%

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

5-chloro-2-nitrobenzyl methanesulfonate结构式

5-chloro-2-nitr...

~%

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

未登录结构式

~%

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

1-溴-3-甲基-2-丁烯结构式

1-溴-3-甲基-2-丁烯

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

~75%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

5-氯-2-硝基苄醇结构式

5-氯-2-硝基苄醇

~%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

DL-缬氨酸甲酯盐酸盐结构式

DL-缬氨酸甲酯盐酸盐

~%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

5-chloro-2-nitrobenzyl methanesulfonate结构式

5-chloro-2-nitr...

~%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

未登录结构式

~%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

(+/-)-methyl 2-[[(2-amino-5-chlorophenyl)methyl]amino]-3-methylbutanoate结构式

(+/-)-methyl 2-...

~%

7-chloro-4-(3-methylbut-2-enyl)-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-4-(3-m...

(+/-)-α-[[(2-amino-5-chlorophenyl)methyl]amino]benzeneacetic acid methyl ester结构式

(+/-)-α-[[(2-am...

~41%

7-chloro-3-phenyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-phen...

5-氯-2-硝基苄醇结构式

5-氯-2-硝基苄醇

~%

7-chloro-3-phenyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-phen...

甲基-2-氨基-2-苯乙酸酯盐酸盐结构式

甲基-2-氨基-2-苯乙酸酯盐酸盐

~%

7-chloro-3-phenyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-phen...

5-chloro-2-nitrobenzyl methanesulfonate结构式

5-chloro-2-nitr...

~%

7-chloro-3-phenyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-phen...

(+/-)-α-[[(5-chloro-2-nitrophenyl)methyl]amino]benzeneacetic acid methyl ester结构式

(+/-)-α-[[(5-ch...

~%

7-chloro-3-phenyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-phen...

5-氯-2-硝基苄醇结构式

5-氯-2-硝基苄醇

~%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

DL-缬氨酸甲酯盐酸盐结构式

DL-缬氨酸甲酯盐酸盐

~%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

5-chloro-2-nitrobenzyl methanesulfonate结构式

5-chloro-2-nitr...

~%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

未登录结构式

~%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

二碳酸二叔丁酯结构式

二碳酸二叔丁酯

7-chloro-3-propan-2-yl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-prop...

~93%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

(+/-)-methyl 2-[[(2-amino-5-chlorophenyl)methyl]amino]-3-methylbutanoate结构式

(+/-)-methyl 2-...

~%

tert-butyl 7-chloro-2-oxo-3-propan-2-yl-3,5-dihydro-1H-1,4-benzodiazepine-4-carboxylate结构式

tert-butyl 7-ch...

7-chloro-3-methyl-1,3,4,5-tetrahydro-1,4-benzodiazepin-2-one结构式

7-chloro-3-meth...

1-溴-3-甲基-2-丁烯结构式

1-溴-3-甲基-2-丁烯

~48%

7-chloro-3-methyl-4-(3-methylbut-2-enyl)-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-3-meth...

未登录结构式

~%

7-chloro-3-methyl-4-(3-methylbut-2-enyl)-3,5-dihydro-1H-1,4-benzodiazepin-2-one结构式

7-chloro-3-meth...