Synthesis, antitubercular and antimicrobial potential of some new thiazole substituted thiosemicarbazide derivatives

被引:43
作者
Abhale, Yogita K. [1 ,2 ]
Shinde, Abhijit [3 ]
Deshmukh, Keshav K. [1 ,2 ]
Nawale, Laxman [4 ]
Sarkar, Dhiman [4 ]
Mhaske, Pravin C. [3 ]
机构
[1] Savitribai Phule Pune Univ, SN Arts DJM Commerce & BNS Sci Coll, Postgrad Dept Chem, Coll Rd, Sangamner 422605, India
[2] Savitribai Phule Pune Univ, SN Arts DJM Commerce & BNS Sci Coll, Res Ctr, Coll Rd, Sangamner 422605, India
[3] Savitribai Phule Pune Univ, Post Grad Dept Chem, SP Mandalis Sir Parashurambhau Coll, Tilak Rd, Pune 411030, Maharashtra, India
[4] Natl Chem Lab, CSIR, CombiChemBio Resource Ctr, Pune 411008, Maharashtra, India
关键词
Thiosemicarbazide; Thiazole; Antitubercular activity; Antimicrobial activity; Cytotoxicity; MYCOBACTERIUM-BOVIS BCG; BIOLOGICAL EVALUATION; INHIBITORS; AGENTS; SEMICARBAZIDE; TUBERCULOSIS; DISCOVERY; DORMANT; DESIGN; SERIES;
D O I
10.1007/s00044-017-1955-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The increase in antibiotic resistance due to multiple factors has warranted the need for search of new compounds which are active against multidrug resistant pathogens. In this context a small focused library of thiosemicarbazide derivatives of 2-arylthiazole-4-carbaldehyde, 4-methyl-2-arylthiazole-5-carbaldehyde and 1-(4-methyl-2-arylthiazol-5-yl) ethanone, (5a-l) has been synthesized. The title compounds were screened for inhibitory activity against Mycobacterium tuberculosis H37Ra (ATCC 25177) and Mycobacterium bovis Bacille Calmette Guerin (ATCC 35743) strains. The synthesized compounds, 5a-l were further assayed for their cytotoxic activity against the two human cancer cell lines, HeLa and human colon carcinoma 116 cell lines and showed no significant cytotoxic activity against these two cell lines at the maximum concentration evaluated. Further, the synthesized compounds were found to have potential antibacterial activity against Gram-negative bacteria, Escherichia coli, Pseudomonas flurescence and Gram-positive bacteria, Staphylococcus aureus, Bacillus subtilis. Most of the synthesized compounds showed moderate activity against fungal strain Candida albicans. This study provides valuable directions to our ongoing endeavor of rationally designing more potent antimycobacterial agent.
引用
收藏
页码:2557 / 2567
页数:11
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