3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis, Mycobacterium tuberculosis CYP121A1 enzyme inhibition and antimycobacterial activity vs drug-sensitive and drug-resistant strains

Claire Simons; Lama A Alshabani; Jabril M Abdali; Alistair Brown; Damião Pergentino de Sousa; Sam Willcocks; Amit Kumar; Ahmed Y.G. Alhejaili; D. Fernando Estrada

doi:10.1039/d5md00738k

January 1, 2026RSC Medicinal ChemistryOpen Access

3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis, Mycobacterium tuberculosis CYP121A1 enzyme inhibition and antimycobacterial activity vs drug-sensitive and drug-resistant strains

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Key Points

The research aims to synthesize compounds that inhibit the CYP121A1 enzyme in Mycobacterium tuberculosis and evaluate their antimycobacterial activity.
Synthesis of 3-(pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives.
Testing of these derivatives for CYP121A1 enzyme inhibition.
Evaluation of the compounds’ efficacy against drug-sensitive and drug-resistant strains of Mycobacterium tuberculosis.
Identified significant inhibition of CYP121A1 by several synthesized derivatives.
Demonstrated effective antimycobacterial activity against both drug-sensitive and drug-resistant strains.

Implication

This research demonstrates the inhibition of CYP121A1 in Mycobacterium tuberculosis, indicating potential against drug-resistant strains.

Abstract

CYP121A1 is a promising cytochrome P450 (CYP) drug target in Mycobacterium tuberculosis (Mtb) owing to its physiological importance in bacterial cell viability. The continuing rise of multidrug resistant (MDR) and...

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Cite This Study

Simons et al. (2026) studied this question.

synapsesocial.com/papers/6985852f8f7c464f23008595 https://doi.org/10.1039/d5md00738k

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3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis, Mycobacterium tuberculosis CYP121A1 enzyme inhibition and antimycobacterial activity vs drug-sensitive and drug-resistant strains

Key Points

Implication

Abstract

Discussion

Cite This Study

3-(Pyridine-3-ylmethylene)chroman-4-one and tetralone derivatives: synthesis, Mycobacterium tuberculosis CYP121A1 enzyme inhibition and antimycobacterial activity vs drug-sensitive and drug-resistant strains

Key Points

Implication

Abstract

Discussion

Cite This Study

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