Fighting Against Resistant Strains: The Case of Benzothiazinones and Dinitrobenzamides

Buroni, Silvia; Riccardi, Giovanna; Pasca, Maria Rosalia

doi:10.5772/29686

Cited by 2 publications

References 40 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Nitroheterocyclics as Anti-Tuberculosis Agents: An Overview

De,

Gupta,

Degani

2024

Frontiers in Drug Design and Discovery

View full text Add to dashboard Cite

Nitroheterocyclics have been used for treating infections since the beginning of the 20th century, however, because of their potential toxicities, they have not been exploited thoroughly, except for a few well known drugs like metronidazole. With the growing threat of multidrug resistant tuberculosis in the last two decades, and interesting preliminary results obtained for nitro heterocyclics, their potential as antituberculosis agents has been realised relatively recently. Thus, after a gap of several decades, nitroheterocyclics are in the forefront amongst the newer scaffolds that have shown utility in treating TB, with five molecules containing the nitro functionality in various phases of clinical trials as well as therapeutic use. Interestingly, these compounds act by multiple different mechanisms of action, and this aspect can be explored further for designing newer molecules. This review presents a detailed discussion of chemical properties of nitro compounds, the importance of which is highlighted in their mechanisms of action as well as toxicity. This is followed by their classification according to the heterocyclic structures, leading to an understanding of mechanisms of action, structure activity relationship and toxicity. Thus, this review about the current status of nitro containing compounds as anti-TB agents could aid in the design of newer molecules containing nitroheterocyclics in the scaffolds, and maintain optimum balance between anti-TB potency and potential toxicity.

show abstract

Nitroheterocyclics as Anti-Tuberculosis Agents: An Overview

De,

Gupta,

Degani

2024

Frontiers in Drug Design and Discovery

View full text Add to dashboard Cite

show abstract

The Anti-Tuberculosis Agents Under Development and the Challenges Ahead

2015

View full text Add to dashboard Cite

Tuberculosis (TB) is a serious health problem causing 1.5 million deaths worldwide. After the discovery of first-line anti-TB drugs, the mortality rate declined sharply, however, the emergence of drug-resistant strains and HIV co-infection have led to increased incidence of this disease. A number of new potential antitubercular drug candidates with novel modes of action have entered clinical trials in recent years. Compounds such as gatifloxacin, moxifloxacin and linezolid, the already known antibiotics are currently being evaluated for their anti-TB activity. OPC-67683 and TMC207 have been approved for the treatment of MDR-TB patients recently, while PA-824, SQ109, PNU-100480, AZD5847, LL3858, SQ609, SQ641, BTZ043, DC-159a, CPZEN-45, Q-203, DNB1, TBA-354 are in various phases of clinical and preclinical developments. This review evaluates the current status of TB drug development and future aspects.

show abstract

Fighting Against Resistant Strains: The Case of Benzothiazinones and Dinitrobenzamides

Cited by 2 publications

References 40 publications

Nitroheterocyclics as Anti-Tuberculosis Agents: An Overview

Nitroheterocyclics as Anti-Tuberculosis Agents: An Overview

The Anti-Tuberculosis Agents Under Development and the Challenges Ahead

Contact Info

Product

Resources

About