ArticleBioorganic & medicinal chemistry2019
Synthesis and biological evaluation of novel cYY analogues targeting Mycobacterium tuberculosis CYP121A1.
Article in Bioorganic & medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed.
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- Synthesis, structural elucidation, and molecular docking of diclofenac-derived hydrazone metal complexes with anti-inflammatory and anticancer potential.Scientific reports · 2025Article
- pH-Dependent Luminescence of Self-Assembly TbChemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Epothilone B from Aspergillus fumigatus with a strong antiproliferative and anti-tubulin polymerizing activities; apoptosis, and cell cycle analyses.BMC microbiology · 2025Article
- Design, Synthesis, Anti-Inflammatory Activity, DFT Modeling and Docking Study of New Ibuprofen Derivatives.International journal of molecular sciences · 2024Article
- Synthesis, biological evaluation and computational studies of pyrazole derivatives asRSC medicinal chemistry · 2022Article
- A Novel Ibuprofen Derivative and Its Complexes: Physicochemical Characterization, DFT Modeling, Docking, In Vitro Anti-Inflammatory Studies, and DNA Interaction.Molecules (Basel, Switzerland) · 2022Article
- Activation modes in biocatalytic radical cyclization reactions.Journal of industrial microbiology & biotechnology · 2021Review
- Evaluation of Luminogenic Substrates as Probe Substrates for Bacterial Cytochrome P450 Enzymes: Application toSLAS discovery : advancing life sciences R & D · 2019Article
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Authors and funding
10 authors.
Funding
Abstract
The rise in multidrug resistant (MDR) cases of tuberculosis (TB) has led to the need for the development of TB drugs with different mechanisms of action. The genome sequence of Mycobacterium tuberculosis (Mtb) revealed twenty different genes coding for cytochrome P450s. CYP121A1 catalyzes a CC crosslinking reaction of dicyclotyrosine (cYY) producing mycocyclosin and current research suggests that either mycocyclosin is essential or the overproduction of cYY is toxic to Mtb. A series of 1,4-dibenzyl-2-imidazol-1-yl-methylpiperazine derivatives were designed and synthesised as cYY mimics. The derivatives substituted in the 4-position of the phenyl rings with halides or alkyl group showed promising antimycobacterial activity (MIC 6.25 μg/mL), with the more lipophilic branched alkyl derivatives displaying optimal binding affinity with CYP121A1 (
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