Redox‐guided small molecule antimycobacterials

Kulkarni, Apoorva; Sharma, Ajay; Chakrapani, Harinath

doi:10.1002/iub.1867

Cited by 4 publications

(3 citation statements)

References 83 publications

(86 reference statements)

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“…Cine addition to target-active hydroxyl intermediates thereby causes the subsequent suicide inhibition of the enzyme . An electron-deficient benzene ring with a thiol produces a Meisenheimer complex that dissociates to generate SO 2 , as shown in Figure . Apart from oxidative stress, carbonic anhydrase inhibitors, dihydropteroate synthase and dihydrofolate reductase inhibition, resistance to the aminoglycoside antibiotic kanamycin A, and an undefined mechanism associated with Wag31 , may be responsible for desired inhibition.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids

et al. 2021

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A series of novel benzhydryl piperazine-coupled nitrobenzenesulfonamide hybrids were synthesized with good to excellent yields. They were tested for in vitro inhibition of mycobacterial activity against the Mycobacterium tuberculosis H37Rv strain, in vitro cytotoxicity MTT (RAW 264.7cells) assay, nutrient starvation (H37Rv strain), and ability to block Cav3.2 T-type calcium channels. Novel hybrids did not inhibit T-type calcium channels, whereas they showed excellent antituberculosis (TB) activity and low cytotoxicity with a selectivity index of >30. A direct impact of the amino acid linker was not observed. Studied hybrids exhibited good inhibition activities, and the 2,4-dinitrobenzenesulfonamide group emerged as a promising scaffold for further drug design by hybridization approaches for anti-TB therapy.

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Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Benzhydrylpiperazine-Coupled Nitrobenzenesulfonamide Hybrids

et al. 2021

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“…29 Small molecules harbouring redox functionalities that can generate ROS to kill drug-resistant Mycobacterium tuberculosis have also been explored. 30…”

Section: Bacterial Signal Transduction Componentsmentioning

confidence: 99%

Chemical Approaches to Tackle the Silent Pandemic of Antibiotic Resistance

2023

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The rapid rise of antibiotic resistance among infectious pathogens is a matter of grave concern. This development of resistance is an evolutionary process, which is intensified due to prolonged and excessive exposure to antibiotics, which will ultimately force us to a situation where well-established lines of treatment will cease to be effective against routine infections. Thus, it is imperative to develop novel strategies to tackle this silent pandemic of antibiotic resistance. Here we briefly summarize the far-reaching implications of antibiotic resistance globally and highlight some key mechanisms by which resistance arises. We also discuss possible approaches to address this problem, including the identification and validation of novel antibacterial pathways that can circumvent existing resistance mechanisms to effectively curb this global threat.

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“…Thus, perturbation of redox-equilibrium can be an effective strategy to induce mycobacterial killing and reverse drug resistance. In the fifth review, Kulkarni et al, (11) present a fascinating overview of redox-based small molecules that have the potential of targeting drug-resistant Mtb. Recent pieces of evidence indicate that reactive oxygen species (ROS) contributes to the killing potential of anti-TB drugs such as rifampicin, clofazimine, and augmentin (12–14).…”

mentioning

confidence: 99%