Synthesis of New 2-Naphthyl Ethers and Their Protective Activities against DNA Damage Induced by Bleomycin-Iron

被引：41

作者：

Abdel-Wahab, Bakr F. ^{[1
]}

El-Ahl, Abdel-Azlz S. ^{[2
]}

Badria, Farid A. ^{[3
]}

机构：

[1] Natl Res Ctr, Appl Organ Chem Dept, Giza, Egypt

[2] Umm Al Qura Univ, Univ Coll Makah, Dept Chem, Mecca, Saudi Arabia

[3] Univ Mansoura, Fac Pharm, Dept Pharmacognosy, Mansoura 35516, Egypt

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2009年 / 57卷 / 12期

关键词：

2-naphthaloxyacetic acids; imidazo[2,1-b]-1,3,4-thiadiazole; pyrazole; hydrazonoyl chloride; 1,3,4-thiadiazole; DNA . bleomycin-iron complex; 1,3,4-OXADIAZOLE DERIVATIVES; ANTIMICROBIAL ACTIVITY; AGENTS; ALPHA; AROYLHYDRAZINES; ANTICONVULSANT;

D O I：

10.1248/cpb.57.1348

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The reaction of 2-naphthaloxyacetic acid with thiosemicarbazide in the presence of phosphoryl chloride, followed by treatment with phenacylbromides, led to the formation of imidazo[2,1-b][1,3,41thiadiazoles 3a-c. 2-(Naphthalen-3-yloxy)acetohydrazide 4 on treatment with ethyl 2-(2-arylhydrazono)-3-oxobutanoates (5a-C), 2-methoxymethylene)malononitrile, or ethyl 2-cyano-3,3-bis(methylthio)acryl ate led to the formation of substituted pyrazoles 6-8. The reaction of the hydrazide 4 with hydrazonoyl chlorides 9a-c and 1,2,4,5-benzene tetracarboxylic- 1,2:4,5-dianhydride produced bis-diazo compounds 10a-c and dimide 11 respectively. All new compounds were tested for their protective activity against DNA damage induced by bleomycin-iron complex. Compound 2 showed the greatest protection against DNA damage, thus diminishing chromogen formation between the damaged DNA and thiobarbituric acid.

引用

页码：1348 / 1351

页数：4

共 39 条

[1] Synthesis and serotonin antagonist and antianexity activities of pyrrolidine derivatives from 4-hydrazinyl-1-p-substituted phenyl-2,5-dihydro-1H-pyrrole-3-carbonitriles [J].