Synthesis, antimicrobial and cytotoxic activities of novel 4-trifluoromethyl-(1,2,3)-thiadiazolo-5-carboxylic acid hydrazide Schiff's bases

被引：9

作者：

Rao, P. Sambasiva ^{[1
]}

Kurumurthy, C. ^{[1
]}

Veeraswamy, B. ^{[1
]}

Kumar, G. Santhosh ^{[1
]}

Narsaiah, B. ^{[1
]}

Kumar, K. Pranay ^{[2
]}

Murthy, U. S. N. ^{[2
]}

Karnewar, Santosh ^{[3
]}

Kotamraju, Srigiridhar ^{[3
]}

机构：

[1] Indian Inst Chem Technol, Fluoroorgan Div, Hyderabad 500607, Andhra Pradesh, India

[2] Indian Inst Chem Technol, Div Biol, Hyderabad 500607, Andhra Pradesh, India

[3] Indian Inst Chem Technol, Chem Biol Div, Hyderabad 500607, Andhra Pradesh, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 04期

关键词：

1,2,3-Thiadiazole; Schiff's bases; Hurd-Mori synthesis; Antibacterial activity; Antifungal activity; Cytotoxic activity; DERIVATIVES; 1,2,3-THIADIAZOLES;

D O I：

10.1007/s00044-012-0168-x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 1,2,3-thiadiazolo-5-carboxylic acid hydrazide Schiff's bases 4a-4r were prepared starting from ethyl-4,4,4-trifluoroacetoacetate and ethyl carbazate in four steps. All the compounds were screened for antibacterial activity against various bacterial strains at 150 mu g/ml concentration and found no activity. Similarly, all the compounds were screened for antifungal activity against various fungal strains at 100 and 150 mu g/ml concentrations. Compounds 4a, 4m, and 4q found to show moderate activity against Candida albicans. Further, compounds were evaluated for cytotoxic activity against breast carcinoma cells MDA-MB 231 (aggressive), MCF-7 (non-aggressive) using doxorubicin as standard. Compound 4n was found to show 25.39 % cell viability against MDA-MB 231 and 63.60 % cell viability against MCF-7 cells.

引用

页码：1747 / 1755

页数：9

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