Literature DB >> 21757344

Novel hybrids of fluconazole and furanones: design, synthesis and antifungal activity.

Hanumant B Borate1, Sangmeshwer P Sawargave, Subhash P Chavan, Mohan A Chandavarkar, Ramki Iyer, Amit Tawte, Deepali Rao, Jaydeep V Deore, Ananada S Kudale, Pankaj S Mahajan, Gopinath S Kangire.   

Abstract

During our efforts to develop new antifungal agents, a number of hybrid molecules containing furanones and fluconazole pharmacophores were designed and synthesized. The new chemical entities thus synthesized were tested for their potential as antifungal agents against various fungal strains and it was observed that the compounds with general structure 7 were potent inhibitors of Candida albicans ATCC 24433, Candida glabrata ATCC 90030, Candida tropicalis ATCC 750 and Candida neoformans ATCC 34664 while the fluconazole analogues 12 exhibited antifungal activity against Candida albicans ATCC 24433 and Candida glabrata ATCC 90030. The structure-activity relationship for these compounds is discussed. The synthetic strategies used in the present work have potential to prepare a large number of compounds for further refinement of structures to obtain molecules suitable for development as antifungal drugs.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21757344     DOI: 10.1016/j.bmcl.2011.06.022

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Design, Synthesis and Evaluation of Bifunctional Acridinine-Naphthalenediimide Redox-Active Conjugates as Antimalarials.

Authors:  Srikanta Dana; Sudhir Kumar Keshri; Jyoti Shukla; Kunwar Somesh Vikramdeo; Neelima Mondal; Pritam Mukhopadhyay; Suman Kumar Dhar
Journal:  ACS Omega       Date:  2016-09-01

Review 2.  The Drug Discovery and Development Industry in India-Two Decades of Proprietary Small-Molecule R&D.

Authors:  Edmond Differding
Journal:  ChemMedChem       Date:  2017-06-01       Impact factor: 3.466

3.  Experimental Examination of Solubility and Lipophilicity as Pharmaceutically Relevant Points of Novel Bioactive Hybrid Compounds.

Authors:  Angelica Sharapova; Marina Ol'khovich; Svetlana Blokhina; German L Perlovich
Journal:  Molecules       Date:  2022-10-01       Impact factor: 4.927

4.  Antifungal activity of synthetic naphthoquinones against dermatophytes and opportunistic fungi: preliminary mechanism-of-action tests.

Authors:  Maria do Perpetuo Socorro Borges Carriço Ferreira; Mariana Filomena do Carmo Cardoso; Fernando de Carvalho da Silva; Vitor Francisco Ferreira; Emerson Silva Lima; João Vicente Braga Souza
Journal:  Ann Clin Microbiol Antimicrob       Date:  2014-07-06       Impact factor: 3.944

  4 in total

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