Synthesis and antimicrobial evaluation of novel 2,4-dihydro-3h-pyrazol-3-one hybrids: a new class of antibiotics.
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Date
2019
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ABSTRACT
The rise in multidrug resistance (MDR) pathogenic microbes has emerged as a critical global health
burden. To address this problem, the scientific community and Pharmaceutical industries worldwide
are focused in developing newer, safer and cost-effective antimicrobial agents. Design and
development of potential antimicrobial agents has been one of the focus areas of the Synthetic and
Medicinal Chemistry Research Group (SMCRG), UKZN. In continuation of the ongoing research in
SMCRG and the need to discover newer antimicrobials, I envisaged to synthesize novel antimicrobial
agents containing 2,4-Dihydro-3H-pyrazol-3-one (pyrazolone) as a core pharmacophoric moiety.
Pyrazolones are versatile heterocyclic building blocks and is a core scaffold in several marketed
drugs such as for analgesic and antipyretic (phenazone, metamizole, propyphenazon, and
remifenazone); neuroprotective agent (edaravon); antispasmodic (dipyron); anti-inflammatory
agents (famprofazone, phenylbutazone, and remifenazone) and more recently there have been several
reports on the pyrazolone analogs as potential antimicrobial agents. In this research work I have
synthesized a series of potential pyrazolone hybrids containing substituted 1,3,4-thiadiazole,
thiazolidinone, triazole, oximes, and chalcones as antimicrobial agents (Figure 1). The work in this
thesis is divided into 7 chapters.
Description
Doctoral Degree. University of KwaZulu-Natal, Durban.