article · Antibiotics
New pyrrolo[1,2-a]quinoline chemical derivatives have been synthesised and tested in the laboratory for activity against tuberculosis. The compounds were screened against both standard laboratory strains and multidrug-resistant strains of Mycobacterium tuberculosis using a microplate assay. Computational methods were also applied to identify potential molecular targets and model molecular docking. Every synthesised derivative demonstrated inhibitory activity against the standard strain at concentrations between 8 and 128 micrograms per millilitre. Among the tested candidates, a specific fluorobenzoyl derivative, compound 4j, exhibited the highest potency, inhibiting the standard strain at 8 micrograms per millilitre and the multidrug-resistant strain at 16 micrograms per millilitre. Computational assessments of pharmacokinetic characteristics further indicated that most of the synthesised compounds possess general drug-like properties, supported by docking analyses showing favourable binding affinities with target bacterial proteins.
Tuberculosis remains a major global health challenge, increasingly complicated by strains that resist standard antibiotic treatments. Identifying new chemical structures capable of inhibiting both drug-susceptible and drug-resistant forms of Mycobacterium tuberculosis is an essential starting point for discovering novel antimicrobial therapies. Demonstrating activity against resistant strains alongside favourable computational drug-likeness highlights promising molecular candidates for addressing stubborn bacterial infections.
The research is at an early discovery stage, presenting newly synthesised chemical entities with validated in vitro efficacy against multidrug-resistant tuberculosis. These compounds could serve as preliminary lead structures for pharmaceutical developers and medicinal chemistry programmes targeting infectious diseases. Significant further work, including in vivo validation, safety profiling, and clinical development, will be required before any therapeutic product can emerge.
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A series of ethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-3-carboxylates <b>4a</b>-<b>f</b> and dimethyl 1-(substituted benzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-2,3-dicarboxylates <b>4g</b>-<b>k</b> have been synthesized and evaluated for their anti-tubercular (TB) activities against H37Rv (American Type Culture Collection (ATCC) strain 25177) and multidrug-resistant (MDR) strains of <i>Mycobacterium tuberculosis</i> by resazurin microplate assay (REMA). Molecular target identification for these compounds was also carried out by a computational approach. All test compounds exhibited anti-tuberculosis (TB) activity in the range of 8-128 µg/mL against H37Rv. The test compound dimethyl-1-(4-fluorobenzoyl)-5-methylpyrrolo[1,2-<i>a</i>]quinoline-2,3-dicarboxylate <b>4j</b> emerged as the most promising anti-TB agent against H37Rv and multidrug-resistant strains of <i>Mycobacterium tuberculosis</i> at 8 and 16 µg/mL, respectively. In silico evaluation of pharmacokinetic properties indicated overall drug-likeness for most of the compounds. Docking studies were also carried out to investigate the binding affinities as well as interactions of these compounds with the target proteins.
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DOI: 10.3390/antibiotics9050233
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