Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy

Cheng, Ya-Juan; Liang, Hua‐Ju; Fang, Cuiting; Zhang, Niu‐niu; Zhang, Tianyu; Yan, Ming

doi:10.3390/molecules24102021

Cited by 5 publications

(6 citation statements)

References 16 publications

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“…Carbamate 115 (Figure ) was published in 2019 as part of a SAR study . This molecule showed an MIC 90 value of 1.8 μM against autoluminescent Mtb H37Ra but had weaker activity against Mtb H37Rv and MDR strains (MICs 11–23 μM) and low cytotoxicity against A549 cells (CC 50 64 μM).…”

Section: Preclinical Promisesmentioning

confidence: 99%

Tuberculosis Drug Discovery: Challenges and New Horizons

et al. 2022

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Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to the 1.8 million deaths caused by COVID-19. The World Health Organization has stated that new TB drugs must be developed to end this pandemic. After decades of neglect in this field, a renaissance era of TB drug discovery has arrived, in which many novel candidates have entered clinical trials. However, while hundreds of molecules are reported annually as promising anti-TB agents, very few successfully progress to clinical development. In this Perspective, we critically review those anti-TB compounds published in the last 6 years that demonstrate good in vivo efficacy against Mycobacterium tuberculosis. Additionally, we highlight the main challenges and strategies for developing new TB drugs and the current global pipeline of drug candidates in clinical studies to foment fresh research perspectives.

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Section: Preclinical Promisesmentioning

confidence: 99%

Tuberculosis Drug Discovery: Challenges and New Horizons

et al. 2022

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“…The results suggest that the steric effect and lipophilicity of the ester group are crucial for antimicrobial activity. It should be noted that compound 6h also exhibited the most potent antitubercular activity in the previous study …”

Section: Resultsmentioning

confidence: 69%

“…In the study of new antitubercular agents, a series of (3‐benzyl‐5‐hydroxyphenyl)carbamates were designed and synthesized. One privileged compound displayed good in vitro and in vivo inhibitory activity against Mycobacterium tuberculosis . During further research, the compound was also found to exhibit potent inhibitory activity against S. aureus .…”

Section: Introductionmentioning

confidence: 97%

Exploration of (3‐benzyl‐5‐hydroxyphenyl)carbamates as new antibacterial agents against Gram‐positive bacteria

Liang

Cheng

Wang

et al. 2020

Archiv der Pharmazie

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A series of (3‐benzyl‐5‐hydroxyphenyl)carbamates were evaluated as new antibacterial agents. Several compounds showed potent inhibitory activity against sensitive and drug‐resistant Gram‐positive bacteria. The compounds are ineffective against all tested Gram‐negative bacteria. The structure of the ester group exerted a profound effect on antibacterial activity. 4,4‐Dimethylcyclohexanyl carbamate 6h exhibited the most potent inhibitory activity against the standard and clinically isolated Staphylococcus aureus, Staphylococcus epidermidis, and Enterococcus faecalis (minimum inhibitory concentration = 4–8 µg/ml) strains. The preliminary experimental evidence indicated that these carbamates target the bacterial cell wall and share a similar mechanism of action with vancomycin.

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“…Herein, the four individual properties MW, log P , HBD, and HBA as well as PSA and ROTB were analyzed for 39 TB drugs (approved and candidates in clinical trials) and 1271 synthetic anti-tubercular compounds reported in 40 publications between 2006 to early 2020. − Instant JChem 17.29.0 [Instant JChem 17.29.0, 2017 ChemAxon Ltd. ()] was used for calculation of physiochemical properties…”

Section: Introductionmentioning

confidence: 99%

Analysis of Approaches to Anti-tuberculosis Compounds

Motamen

Quinn

2020

ACS Omega

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Mycobacterium tuberculosis (Mtb) remains a deadly pathogen two decades after the announcement of tuberculosis (TB) as a global health emergency by the World Health Organization. Medicinal chemistry efforts to synthesize potential drugs to shorten TB treatments have not always been successful. Here, we analyze physiochemical properties of 39 TB drugs and 1271 synthetic compounds reported in 40 publications from 2006 to early 2020. We also propose a new TB space of physiochemical properties that may provide more appropriate guidelines for design of anti-TB drugs.

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Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy

Cited by 5 publications

References 16 publications

Tuberculosis Drug Discovery: Challenges and New Horizons

Tuberculosis Drug Discovery: Challenges and New Horizons

Exploration of (3‐benzyl‐5‐hydroxyphenyl)carbamates as new antibacterial agents against Gram‐positive bacteria

Analysis of Approaches to Anti-tuberculosis Compounds

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