What question did this study set out to answer?

To design, synthesize, and evaluate novel thiazolo[5,4-b]pyridine–sulfonamide conjugates for antimicrobial efficacy and characterize their structure–activity relationships and binding modes.

August 16, 2026Arabian Journal of ChemistryOpen Access

Novel thiazolo5,4-bpyridine–sulfonamide conjugates: Synthesis, structure–activity relationship, and molecular docking studies

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Authors

NANoof A. Alenazi

Discussion

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Overview

In vitro study reveals potent antimicrobial activity of novel thiazolopyridine–sulfonamide hybrids, highlighting their potential as dihydrofolate reductase inhibitors.

Key Points

To design, synthesize, and evaluate novel thiazolo[5,4-b]pyridine–sulfonamide conjugates for antimicrobial efficacy and characterize their structure–activity relationships and binding modes.
Synthesized a series of thiazolo[5,4-b]pyridine–sulfonamide hybrid derivatives using a cyanoacetyl sulfonamide intermediate.
Evaluated in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Candida albicans using agar diffusion and minimum inhibitory concentration (MIC) assays.
Performed molecular docking simulations targeting dihydrofolate reductase (DHFR, PDB ID: 2W9S) to assess binding affinity and intermolecular interactions.
Several synthesized conjugates demonstrated potent antimicrobial action, with MIC values ranging between 3.125 and 12.5 μg/mL, with compounds 10, 16, and 21 displaying broad-spectrum activity comparable or superior to reference agents.
Structure–activity relationship analysis established that introducing electron-withdrawing and aromatic substituents significantly enhanced antimicrobial potency.
Molecular docking against DHFR confirmed strong binding affinities and favorable binding interactions for the most active hybrid derivatives.

Cite This Study

Noof A. Alenazi (2026) studied this question.

synapsesocial.com/papers/6a817ab4f2fb91fc834aebf0 https://doi.org/10.25259/ajc_65_2026

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August 16, 2026Arabian Journal of ChemistryOpen Access

Novel thiazolo5,4-bpyridine–sulfonamide conjugates: Synthesis, structure–activity relationship, and molecular docking studies

View Full Paper

Ask AI

Bookmark

Authors

NANoof A. Alenazi

Discussion

Member takes

Overview

In vitro study reveals potent antimicrobial activity of novel thiazolopyridine–sulfonamide hybrids, highlighting their potential as dihydrofolate reductase inhibitors.

Key Points

To design, synthesize, and evaluate novel thiazolo[5,4-b]pyridine–sulfonamide conjugates for antimicrobial efficacy and characterize their structure–activity relationships and binding modes.
Synthesized a series of thiazolo[5,4-b]pyridine–sulfonamide hybrid derivatives using a cyanoacetyl sulfonamide intermediate.
Evaluated in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, and Candida albicans using agar diffusion and minimum inhibitory concentration (MIC) assays.
Performed molecular docking simulations targeting dihydrofolate reductase (DHFR, PDB ID: 2W9S) to assess binding affinity and intermolecular interactions.
Several synthesized conjugates demonstrated potent antimicrobial action, with MIC values ranging between 3.125 and 12.5 μg/mL, with compounds 10, 16, and 21 displaying broad-spectrum activity comparable or superior to reference agents.
Structure–activity relationship analysis established that introducing electron-withdrawing and aromatic substituents significantly enhanced antimicrobial potency.
Molecular docking against DHFR confirmed strong binding affinities and favorable binding interactions for the most active hybrid derivatives.

Cite This Study

Noof A. Alenazi (2026) studied this question.

synapsesocial.com/papers/6a817ab4f2fb91fc834aebf0 https://doi.org/10.25259/ajc_65_2026

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