Synthesis, anti microbial screening and cytotoxic studies of some novel pyrazole analogs

نویسندگان

  • K. Sony Jacob
  • Swastika Ganguly
چکیده

Article history: Received on: 29/07/2016 Revised on: 21/08/2016 Accepted on: 11/09/2016 Available online: 29/11/2016 The objective of the study was to synthesize novel pyrazole analogs and evaluate their antimicrobial, anthelmintic and cytotoxic activity. Novel (Z)-1-(4-chlorophenyl)-2-(3,5-dimethyl-4-(substituited phenyldiazenyl)-1H-pyrazol-1-yl)ethanone derivatives were synthesized by conventional method using potassium carbonate in DMF, under reflux condition. The antibacterial study was carried out against gram positive and gram negative bacteria using ciprofloxacin and norfloxacin as standard drugs. Antifungal activity was compared against fluconazole and evaluated using Candida albicans (MTCC 227) and Aspergillus niger (NCIM 1056). Anthelmentic activity assay was carried out on Indian earthworm, Pheretima posthuma. In vitro cytotoxicity studies were also carried out using Dalton’s lymphoma ascites cells (DLA) and Ehrlich ascites carcinoma cells (EAC). Results of antibacterial study indicated that the compound 22 showed most promising activity against both Gram-positive and Gram-negative organisms. Compound 21 and 24, exhibited relatively good inhibitory profile against Gram negative organism. In case of compounds 25,27-30 exhibited equally potent antifungal activity as that of the standard drug fluconazole. Moreover, compound 21-24,26 showed excellent activity against C. albicans and A.niger. The in vitro cytotoxicity results and anthelmintic reports indicated compound 22 exhibited promising activity among the tested analogs. These newly synthesized pyrazole analogs, especially 21, 22 and 24 are better scaffolds to develop as broad spectrum chemotherapeutic agents.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and Evaluation of New Fluorinated Anti-Tubercular Compounds

Treatment of tuberculosis (TB) and the discovery of effective new anti tubercular drugs is one of the most urgent priorities in health organizations all around the world. In the present study, fluorinated analogs of some of the most important anti-TB agents such as p-aminosalicylic acid (PAS), thiacetazone and pyrazinamide were synthesized and tested against TB. The fluorinated analog of thiace...

متن کامل

Synthesis and Evaluation of New Fluorinated Anti-Tubercular Compounds

Treatment of tuberculosis (TB) and the discovery of effective new anti tubercular drugs is one of the most urgent priorities in health organizations all around the world. In the present study, fluorinated analogs of some of the most important anti-TB agents such as p-aminosalicylic acid (PAS), thiacetazone and pyrazinamide were synthesized and tested against TB. The fluorinated analog of thiace...

متن کامل

Synthesis and Cytotoxic Evaluation of Some Novel Sulfonamide Derivatives Against a Few Human Cancer Cells

Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel...

متن کامل

Synthesis and Cytotoxic Evaluation of Some Novel Sulfonamide Derivatives Against a Few Human Cancer Cells

Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel...

متن کامل

Synthesis Pyrano [2,3-c] Pyrazole-based compounds to induce apoptosis by reducing the expression of anti-apoptotic Bcl-2 protein in human breast cancer MCF-7 cells

Aim: Bcl-2 is a potential target for tumor treatment. The inhibition of the Bcl-2 production is research target of attract in the field of anti-cancer drug development. Recently, the assessment of antitumor activity appeared to be promising for pyrazole derivatives. Therefore, this study was designed to investigate the anti-cancer effects of novel pyrazole derivatives (HN1and HN2.). Material an...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:

دوره   شماره 

صفحات  -

تاریخ انتشار 2016