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Combinatorial approach: identification of potential antifungals from triazole minilibraries

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Abstract

Employing basic principles of solution phase combinatorial chemistry, a solution phase combinatorial synthesis and screening of mini libraries of 1,2,4-triazole derivatives has been carried out. 6 × 6 indexed mini libraries were synthesized comprising of 36 compounds. The libraries were analyzed by liquid chromatography–mass spectrometry–mass spectrometry (LC–MS–MS) analysis. All the synthesized mini libraries were screened for antifungal activity and by deconvolution methodology leads for every fungi used for study were identified. The leads were synthesized individually and screened for activity. The antifungal activity of individually synthesized leads was improved as anticipated, in comparison with that of any of the mini libraries.

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Acknowledgment

The authors are thankful to the Principal, Bharati Vidyapeeth College of Pharmacy, Kolhapur for providing necessary facilities for this work.

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  1. Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Near Chitranagri, Kolhapur, 416013, Maharashtra, India

    Manish Sudesh Bhatia, Bandu Eknath Zarekar, Prafulla Balkrishna Choudhari, Kundan Bhanudas Ingale & Neela Manish Bhatia

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  1. Manish Sudesh Bhatia
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  2. Bandu Eknath Zarekar
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  3. Prafulla Balkrishna Choudhari
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  4. Kundan Bhanudas Ingale
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  5. Neela Manish Bhatia
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Correspondence to Manish Sudesh Bhatia.

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Bhatia, M.S., Zarekar, B.E., Choudhari, P.B. et al. Combinatorial approach: identification of potential antifungals from triazole minilibraries. Med Chem Res 20, 116–120 (2011). https://doi.org/10.1007/s00044-009-9283-8

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