Literature DB >> 19640616

Synthesis, characterization and antibacterial activity of 2-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-5-(substituted-phenyl)-[1,3,4]oxadiazoles.

Neithnadka Premsai Rai1, Venugopala Katharigatta Narayanaswamy, Sheena Shashikanth, Pirama Nayagam Arunachalam.   

Abstract

In the present investigation a series of novel 2-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-5-(substituted-phenyl)-[1,3,4]oxadiazoles (4a-j) were synthesized by cyclization of substituted-benzoic acid N'-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazole-4-carbonyl]-hydrazide by using phosphorousoxychloride at 120 degrees C. The chemical structure of the newly synthesized compounds was characterized by analytical and spectral (IR, (1)H NMR, (13)C NMR and LC-MS) methods. The title compounds were screened for qualitative (zone of inhibition) and quantitative antibacterial activity (MIC) by agar cup plate and microtitration methods, respectively. Among the synthesized compounds in this series compound 2-[1-(5-chloro-2-methoxyphenyl)-5-methyl-1H-pyrazol-4-yl]-5-(4-fluorophenyl)-1,3,4-oxadiazole (4b) was found to exhibit significant antibacterial activity with MICs of 22.4, 29.8, 29.6 and 30.0 microg/mL against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Klebsiella pneumoniae, respectively. The other compounds exhibited moderate activity when compared to standard substance Ampicillin.

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Year:  2009        PMID: 19640616     DOI: 10.1016/j.ejmech.2009.06.020

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Synthesis, X-ray crystal structures and optical properties of novel substituted pyrazoly 1,3,4-oxadiazole derivatives.

Authors:  Hong-Shui Lv; Yong-Sheng Xie; Wei-Yong Liu; Zhong-Liang Gong; Bao-Xiang Zhao
Journal:  J Fluoresc       Date:  2011-03-05       Impact factor: 2.217

2.  4-[(Anthracen-9-yl-methyl-idene)amino]-1,5-dimethyl-2-phenyl-1H-pyrazol-3(2H)-one.

Authors:  Abdullah M Asiri; Salman A Khan; M Nawaz Tahir
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-30

3.  Ethyl 1-cyclo-hexyl-5-(4-meth-oxy-phen-yl)-1H-pyrazole-4-carboxyl-ate.

Authors:  Hoong-Kun Fun; Ching Kheng Quah; B Chandrakantha; A M Isloor; Prakash Shetty
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-11-30
  3 in total

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