Journal: Journal of Pharmacy Research

Article Id: JPRS-PC-00001523
Title: Synthesis, in vitro antifungal and antitubercular evaluation of novel amino pyrimidines based tetrazole derivatives
Category: Pharmaceutical Chemistry
Section: Research Article
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    Aims: The aim of the present study is to synthesis of  novel series of  4-(4-(1H-tetrazole-1-yl) aryl) -6-phenylpyrimidine-2-amines(8a-i)  and screening for their invitro antifungal  and anti tubercular activities. Methods: The compounds (8a-i) has been synthesized by 1-(4-(1H-tetrazole-1-yl) phenyl)-3-arylprop-2-en-1-ones (7a-i) with guanidine nitrate under the basic condition. The compounds are characterized by melting point, elemental analysis FT-IR, MS, 1H and 13C NMR spectroscopic data. The synthesized compounds were screened for in vitro anti-fungal and anti-tubercular activity against their microorganisms. Results: Compounds 8b, 8e and 8i are proved to be more potent against fungal strains when compared with the standard. 8i at a concentration of 10µg/ml showed inhibition against the growth of M. tuberculosis and it is emerged as lead molecule showing excellent activities, against a panel of microorganisms. These effective results also supported by in silico molecular docking study using 14a-demethylase (1E9X) protein. Conclusion: The compounds 8b, 8e and 8i exhibited maximum invitro antifungal and antitubercular activities against different strains. Thus in future, this kind of pyrimidine derivatives may be used to generate better drugs with improved antifungal and tuberculosis activities.

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    Author(s) Name:

    Sandhirakasu Vembu1, Pavadai Parasuraman2, Mannathusamy Gopalakrishnan1*

    Affiliation(s) Name:

    1Department of Chemistry, Annamalai University, Annamalai Nagar, Chidambaram-608002, Tamil Nadu, India
    2Department of Pharmacy, Annamalai University, Annamalai Nagar, Chidambaram-608002, Tamil Nadu, India

    *Corresponding author.
    Professor Dr. M. Gopalakrishnan M.Sc., Ph.D.,
    Department of Chemistry,
    Annamalai University,
    Annamalai Nagar,
    Chidambaram-608002, Tamil Nadu, India.

    Received on:14-08-2014; Revised  on: 22-09-2014; Accepted on:26-10-2014

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    Author:

    Sandhirakasu Vembu1, Pavadai Parasuraman2, Mannathusamy Gopalakrishnan1*

    Title:Synthesis, in vitro antifungal and antitubercular evaluation of novel amino pyrimidines based tetrazole derivatives
    Journal:Journal of Pharmacy Research
    Vol(issue):8 (October)
    Year:2014
    Page No: (1552-1558)
  • Experimental Methods Keywords

    Methodology:anti-tubercular; anti-fungal; 14alpha-demethylase.
    Research Materials:1-H tetrazole; pyrimidine-2-amines

Keywords

1-H tetrazole; pyrimidine-2-amines; anti-tubercular; anti-fungal; 14alpha-demethylase.

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