Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 14, Pages 3079-3083Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.018
Keywords
4-Nitropyrrole; Semicarbazides; Thiosemicarbazides; Antimicrobial agent; Anti-tubercular agent
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Funding
- College of Health Science, University of KwaZulu-Natal, Durban, South Africa
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We report the synthesis and screening of forty novel 4-nitropyrrole-semicarbazide conjugates inspired from the reported bio-potential of bromopyrrole alkaloids and semicarbazide derivatives for antimicrobial activity. Herein, hybrids 5k-5o, 5r, 5s and 5t displayed four-fold increased activity (MIC = 0.39 mu g/mL) against Escherichia coli compared to standard ciprofloxacin. Eight hybrids, 5k-5o and 5r-5t displayed equal antibacterial activity (MIC = 1.56 mu g/mL) against Klebsiella pneumonia compared to standard ciprofloxacin. Hybrid, 5k-5o (MIC = 0.195 mu g/mL) displayed highly potent antibacterial activity against MSSA as compared to standard ciprofloxacin. Eight-fold superior activity was observed for four hybrids 5k-5m and 5o (MIC = 0.391 mu g/mL) against MRSA. Further, nine hybrids displayed four-fold superior antifungal activity (MIC = 0.78 mu g/mL) compared to standard Amphotericin B. Encouraging MICs of these hybrids recognize them as promising leads for development of potential antimicrobial drugs. (C) 2014 Elsevier Ltd. All rights reserved.
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