Tanzania
Research Article
Boronic-aurone Derivatives as Anti-Tubercular Agents: Design, Synthesis and Biological Evaluation
Author(s): Francis E Umesiri, Ashley Lick, Christine Fricke and Thomas I NathanielFrancis E Umesiri, Ashley Lick, Christine Fricke and Thomas I Nathaniel
Purpose: Current study involved the design, synthesis and biological evaluation of novel boronic-aurones as anti-tubercular agents targeting inhibition of antigen 85, enzymatic complex involved in synthesis of mycobacterial cell wall. To minimize the probability of a single mutation leading to resistance, it is important to target multiple enzymes implicated in mycobacterium cell wall biosynthesis. Hence, new synthetics were virtually screened against both antigen 85 and enoyl-[acyl-carrier-protein] reductase (InhA).
Methods: Using a structure-based approach, new boronic aurone derivatives were designed to target both antigen 85 and InhA, synthesized and screened for anti-tuberculosis activity against Mycobacterium smegmatis. Minimum inhibitory concentration(MIC) was determined using resazurin-.. Read More»
DOI:
10.4172/2161-0444.1000297
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