News on therapeutic management of MDR-tuberculosis: a literature review

Barthod, Lucie; Lopez, Jean-Guillaume; Curti, Christophe; Bornet, Corinne; Roche, Manon; Montana, Marc; Vanelle, Patrice

doi:10.1080/1120009x.2017.1338845

Cited by 9 publications

(9 citation statements)

References 84 publications

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“…Despite these analogues displaying enhanced antimycobacterial activity in vitro and in vivo, levofloxacin was shown to be more cost-effective, and therefore more accessible in resource-limited high burden settings [18]. In comparison to moxifloxacin, gatifloxacin and levofloxacin, DC-159a, a relatively new fluoroquinolone analogue was shown to exhibit enhanced bactericidal activity against MDR-TB both in vitro and in vivo and may therefore be a promising new therapeutic candidate for reducing treatment time for both MDR-and drug-sensitive (DS)-TB [22,23].…”

Section: Moxifloxacin Gatifloxacin Levofloxacin and Dc-159amentioning

confidence: 99%

Drug Repurposing for Tuberculosis

Cardoso¹,

Oosthuizen²,

Peton³

et al. 2022

Drug Repurposing - Molecular Aspects and Therapeutic Applications

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Tuberculosis (TB), caused by Mycobacterium tuberculosis, is a major global health concern given the increase in multiple forms of drug-resistant TB. This underscores the importance of a continuous pipeline of new anti-TB agents. From recent studies, it is evident that the increase in drug efficacy is being achieved through re-engineering old TB-drug families and repurposing known drugs. This approach has led to producing a newer class of compounds which not only saves time and investment in developing newer drugs but is also effective in identifying drug candidates with novel mechanisms to treat multi-drug resistant strains. The repurposed drugs moxifloxacin, linezolid, and clofazimine are used to treat extensively drug-resistant TB when first- and/or second-line drugs fail. The chapter covers a detailed background on the current status of the repurposed drugs in the TB drug-discovery pipeline and discusses a potential way forward.

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Section: Moxifloxacin Gatifloxacin Levofloxacin and Dc-159amentioning

confidence: 99%

Drug Repurposing for Tuberculosis

Cardoso¹,

Oosthuizen²,

Peton³

et al. 2022

Drug Repurposing - Molecular Aspects and Therapeutic Applications

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“…In 2020, the World Health Organization estimated that about 10 million people (range: 8.9–11.0 million) contracted tuberculosis (TB) in 2019, which was responsible for 1.4 million deaths [ 1 ]. Treatment of drug-susceptible active tuberculosis consists of a standard 6-month regimen of four antimicrobials (usually isoniazid, rifampin, pyrazinamide, and ethambutol) [ 2 , 3 ]. However, these regimens are lengthy, only partially effective, and associated with high rates of adverse events.…”

Section: Introductionmentioning

confidence: 99%

Quinoxaline Moiety: A Potential Scaffold against Mycobacterium tuberculosis

et al. 2021

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Background. The past decades have seen numerous efforts to develop new antitubercular agents. Currently, the available regimens are lengthy, only partially effective, and associated with high rates of adverse events. The challenge is therefore to develop new agents with faster and more efficient action. The versatile quinoxaline ring possesses a broad spectrum of pharmacological activities, ensuring considerable attention to it in the field of medicinal chemistry. Objectives. In continuation of our program on the pharmacological activity of quinoxaline derivatives, this review focuses on potential antimycobacterial activity of recent quinoxaline derivatives and discusses their structure–activity relationship for designing new analogs with improved activity. Methods. The review compiles recent studies published between January 2011 and April 2021. Results. The final total of 23 studies were examined. Conclusions. Data from studies of quinoxaline and quinoxaline 1,4-di-N-oxide derivatives highlight that specific derivatives show encouraging perspectives in the treatment of Mycobacterium tuberculosis and the recent growing interest for these scaffolds. These interesting results warrant further investigation, which may allow identification of novel antitubercular candidates based on this scaffold.

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“…Additionally, new generation of quinolone derivative, TBK 613, has also shown promising antitubercular activity (Spigelman, 2008) with possible efficacy against fluoroquinolone-resistant strains (Maitra et al, 2015). Another molecule of quinolone family, DC-159a, was DNA gyrase A inhibitor that demonstrated dose-dependent bactericidal activity and MIC 90 was found to be 8 times lower than MFX (moxifloxacin) (Barthod et al, 2017). Bogatcheva et al (2011) reported the identification of SQ609 as a lead compound from a library of dipiperidines.…”

Section: Introductionmentioning

confidence: 99%

Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches

2021

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Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis (Mtb) and one of the deadliest infectious diseases in the world. Mtb has the ability to become dormant within the host and to develop resistance. Hence, new antitubercular agents are required to overcome problems in the treatment of multi-drug-resistant Tb (MDR-Tb) and extensively drug-resistant Tb (XDR-Tb) along with shortening the treatment time. Several efforts are being made to develop very effective new drugs for Tb, within the pharmaceutical industry, the academia and through public-private partnerships. This review will address the antitubercular activities, biological target, mode of action, synthetic approaches and thoughtful concept for the development of several new drugs currently in the clinical trial pipeline (up to October 2019) for tuberculosis. The aim of this review may be very useful in scheming new chemical entities (NCEs) for Mtb.

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News on therapeutic management of MDR-tuberculosis: a literature review

Cited by 9 publications

References 84 publications

Drug Repurposing for Tuberculosis

Drug Repurposing for Tuberculosis

Quinoxaline Moiety: A Potential Scaffold against Mycobacterium tuberculosis

Novel candidates in the clinical development pipeline for TB drug development and their synthetic approaches

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