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Inventi Impact - Pharm Biotech & Microbio

Articles

  • Inventi:pbm/24194/17
    PERSPECTIVES OF 2-(P-HYDROXYPHENYL)-4-(SUBSTITUTED-PHENYL)- 1H-1,5-BENZODIAZEPINES AS EMERGING CLASS OF ANTI-FUNGAL CANDIDATES
    Animeshchandra G M Haldar, Santosh S Chhajed, Kanhiya M Dadure, Debarshi Kar Mahapatra*

    The present research involved screening of anti-fungal potentials of some 2-(p-hydroxyphenyl)-4–(substitutedphenyl)- 1H-1,5–benzodiazepine derivatives against Candida albicans (C. albicans, MTCC 227), Aspergillus niger (A. niger, MTCC 277) and Aspergillus flavus (A. flavus, MTCC 418). The compounds were previously reported by our group and the structures were established by sophisticated analytical techniques. The produced BZD derivatives presented a very promising anti-fungal activity. The fabricated candidates (1a-j) exhibited the zone of inhibition (ZOI) in the range of 17-28 mm against all the three species. The log P (lipophilicity) remained a key factor for the biological activity. The compound 1e (2-(4’-hydroxyphenyl)-4-(4”- fluorophenyl)-1H-1,5-benzodiazepine) containing 2-fluoro substituent has demonstrated the highest activity with a zone of inhibition of 28 mm at MIC of 25 μg/ml. The study establishes a crystal clear structure-activity relationship (SAR) where it was found that electron withdrawing groups are essential in 1,5-BZD scaffold to exhibit fungicidal activity against C. albicans, A. niger and A. flavus. The molecules do hold the perspective to be utilized as clinical candidates in future after suitable evaluation.

    How to Cite this Article
    Animeshchandra G M Haldar, Santosh S Chhajed, Kanhiya M Dadure et al. Perspectives of 2-(p-hydroxyphenyl)-4-(substituted-phenyl)-1H-1,5- benzodiazepines as Emerging Class of Anti-Fungal Candidates. Inventi Impact: Pharm Biotech & Microbio, 2018(1):15-17, 2018.
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