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Design, synthesize, and evaluate a novel series of thiazole derivatives bearing a pyridine moiety for antimicrobial efficacy and DNA gyrase inhibition.

April 12, 2021Scientific ReportsOpen Access

Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents

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Authors

RKRizk E. KhidreNational Research Centre IRIbrahim Ali M. RadiniJazan University

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Implication

In vitro study demonstrates potent antimicrobial activity and DNA gyrase binding of novel thiazole-pyridine derivatives, suggesting potential as therapeutic antimicrobial agents.

Key Points

Design, synthesize, and evaluate a novel series of thiazole derivatives bearing a pyridine moiety for antimicrobial efficacy and DNA gyrase inhibition.
Synthesized substituted dihydropyridine-3-carbonitrile derivatives via reactions of a thiourea precursor with various halogenated electrophiles.
Evaluated target binding in silico via molecular docking simulations against DNA gyrase and assessed in vitro antimicrobial efficacy via minimum inhibitory concentration (MIC) assays.
Synthesized novel thiazole derivatives demonstrated in silico docking scores ranging between -6.4 and -9.2 kcal/mol against DNA gyrase.
Compound 13a exhibited antibacterial activity with MIC values ranging from 46.9 to 93.7 μg/mL and antifungal activity with MIC values from 5.8 to 7.8 μg/mL.

Cite This Study

Khidre et al. (2021) studied this question.

synapsesocial.com/papers/6a0df28188250cfcc2a540f2 https://doi.org/10.1038/s41598-021-86424-7

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Implication

In vitro study demonstrates potent antimicrobial activity and DNA gyrase binding of novel thiazole-pyridine derivatives, suggesting potential as therapeutic antimicrobial agents.

Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents

Discussion

Member takes

Implication

Key Points

Cite This Study

Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents

Discussion

Member takes

Implication

Key Points

Cite This Study

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