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Asian Journal of Research in Chemistry
Year : 2015, Volume : 8, Issue : 8
First page : ( 511) Last page : ( 520)
Print ISSN : 0974-4169. Online ISSN : 0974-4150.
Article DOI : 10.5958/0974-4150.2015.00081.4

Target Oriented Selective Synthesis of Antibacterial Active Tyrosinase Enzyme Inhibitor Coumarin Core Derivatives

Kumbhar Digambar1, Patil Reshma1, Patil Dayanand2, Patravale Ajinkya2, Chandam Dattatray2, Jadhav Sunetra1, Chavan Dattatray2, Choudhari Prafulla3, Bhatia Manish3, Deshmukh Madhukar1,2,*

1Department of Agrochemicals and Pest Management, Shivaji University, Kolhapur, Maharashtra, India

2Department of Chemistry, Shivaji University, Kolhapur, Maharashtra, India

3Computational Drug Discovery Lab Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur, Maharashtra, India

*Corresponding Author E-mail: shubhlaxmi111@gmail.com

Online published on 17 October, 2015.

Abstract

Target oriented designs and selective synthesis of bioactive molecules with broad spectrum activity is a challenging job in the field of modern organic chemistry. Considering this opportunity herein, we report a highly competent selective synthesis of bioactive coumarin core derivative. Using computational drug design software only four selective antibacterial active derivatives was discovered and then synthesized. The efficiency of the synthesized compounds was scrutinized against bacterial pathogens such as P. vulgaris and B. megaterium. All the synthesized compounds showed better theoretical as well as practical results against selected pathogenic species. The minimum inhibitory concentration (MIC) values of the most active heterocycles were compared with that of ciprofloxacin. Results obtained in tyrocinase inhibition assay exactly correlate with MIC results and docking outcomes. The bioactivity of these type moieties provided a novel approach to develop new types of antibacterial drugs like entities effective against pathogens.

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Keywords

Docking simulation, Coumarin aldehyde, Cyclic 1, 3-diketone, Acetic acid medium, Antibacterial activity, MIC, Tyrocinase inhibition assay.

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