Literature DB >> 21689870

Synthesis, antibacterial evaluation and QSAR studies of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolone derivatives.

Rajnish Kumar1, Ashwani Kumar, Sandip Jain, Darpan Kaushik.   

Abstract

A series of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolones (I-XXI) were synthesized using an appropriate synthetic route and characterized by elemental and spectral analysis. The antibacterial activities of all the synthesized compounds were evaluated against identifiable bacterial strains. Compounds III, IV, VII, VIII, IX, X, XI, XV, &XVIII showed better activity than parent compound against all the selected strains. QSAR study on the synthesized molecules tested for their antibacterial activity was performed using multiple linear regression method. Generated models revealed a decrease in HOMO energy as favorable descriptor for determining and predicting the antibacterial activity of the synthesized compounds. Further, the developed models were cross validated using LOO method for their predictive nature.
Copyright © 2011. Published by Elsevier Masson SAS.

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Year:  2011        PMID: 21689870     DOI: 10.1016/j.ejmech.2011.04.035

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


  3 in total

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Review 3.  Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Authors:  Cledualdo Soares de Oliveira; Bruno Freitas Lira; José Maria Barbosa-Filho; Jorge Gonçalo Fernandez Lorenzo; Petrônio Filgueiras de Athayde-Filho
Journal:  Molecules       Date:  2012-08-27       Impact factor: 4.411

  3 in total

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