Quinoline and quinolones: promising scaffolds for future antimycobacterial agents

Singh, Sandeep; Kaur, Gurpuneet; Mangla, Veenu; Gupta, Maneesh K.

doi:10.3109/14756366.2014.930454

Cited by 69 publications

(28 citation statements)

References 51 publications

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“…9 Incidentally, 2-(quinolin-4-yloxy)acetamides have been described as noncytotoxic compounds endowed with potent inhibitory activity against M. tuberculosis H37Rv in vitro. 10 These molecules were obtained from phenotypic screening leading to a set of 177 lead-compounds.…”

mentioning

confidence: 99%

2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

Pissinate

Villela

Rodrigues-Junior

et al. 2016

ACS Med. Chem. Lett.

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2-(Quinolin-4-yloxy)acetamides have been described as potent in vitro inhibitors of Mycobacterium tuberculosis growth. Herein, additional chemical modifications of lead compounds were carried out, yielding highly potent antitubercular agents with minimum inhibitory concentration (MIC) values as low as 0.05 μM. Further, the synthesized compounds were active against drug-resistant strains and were devoid of apparent toxicity to Vero and HaCat cells (IC 50 s ≥ 20 μM). In addition, the 2-(quinolin-4-yloxy)acetamides showed intracellular activity against the bacilli in infected macrophages with action similar to rifampin, low risk of drug−drug interactions, and no sign of cardiac toxicity in zebrafish (Danio rerio) at 1 and 5 μM. Therefore, these data indicate that this class of compounds may furnish candidates for future development to, hopefully, provide drug alternatives for tuberculosis treatment.

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confidence: 99%

2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

Pissinate

Villela

Rodrigues-Junior

et al. 2016

ACS Med. Chem. Lett.

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“…Quinoline and derivatives represent an important class of heterocyclic in the medicinal chemistry field because its wide range of biological activities, including antituberculosis [35]. Machado and coworkers have reported a series of quinoline derivatives with inhibitory activity against a clinical isolate of an MDR-TB strain.…”

Section: Antituberculosis Compoundsmentioning

confidence: 99%

Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds

2017

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Tuberculosis (TB), a disease caused mainly by the Mycobacterium tuberculosis (Mtb), is according to the World Health Organization (WHO) the infectious disease responsible for the highest number of deaths worldwide. The increased number of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains, and the ineffectiveness of the current treatment against latent tuberculosis are challenges to be overcome in the coming years. The scenario of drug discovery becomes alarming when it is considered that the number of new drugs does not increase proportionally to the emergence of drug resistance. In this review, we will demonstrate the current advances in antitubercular drug discovery, focusing on the research of compounds with potent antituberculosis activity against MDR-TB strains. Herein, active compounds against MDR-TB with minimum inhibitory concentrations (MICs) less than 11 µM and low toxicity published in the last 4 years in the databases PubMed, Web of Science and Scopus will be presented and discussed.

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“…Fluoroquinolones (FLQs) are synthetic antibiotics originated from quinolone and its derivatives 6 . FLQs show a 4-quinolone core and 3-and 4-carboxy carbonyl pending chains, which mediated the antibacterial activity.…”

Section: Introductionmentioning

confidence: 99%

Microextraction by packed sorbent and HPLC–PDA quantification of multiple anti-inflammatory drugs and fluoroquinolones in human plasma and urine

D’Angelo

Tessari

Bellagamba

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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We developed and validated an analytical method based on microextraction packed sorbent (MEPS) and high-performance liquid chromatography (HPLC) coupled to photodiode array (PDA) detector to simultaneously quantify multiple nonsteroidal anti-inflammatory drugs (NSAIDs) and fluoroquinolones (FLQs), which may provide as combination several adverse reactions in nephrology and neurology. The linearity range from LOQs (0.1 μg/mL) to 10 μg/mL, and LODs values were 0.03 μg/mL for both NSAIDs and FLQs. The validation was performed according to international guidelines and the accuracy was tested measuring the precision, intermediate precision and trueness. The drugs stability was tested under different storage conditions (+4 °C and -20 °C) and after three different cycles of freezing and thawing. The method can be a suitable tool to simultaneously detect a possible association of drugs in human biological samples and provide several potentialities for clinical applications, bioequivalence studies, pharmacodynamics and toxicodynamics of different pharmaceutical dosage forms showing NSAIDs and FLQs.

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Quinoline and quinolones: promising scaffolds for future antimycobacterial agents

Cited by 69 publications

References 51 publications

2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains

Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds

Microextraction by packed sorbent and HPLC–PDA quantification of multiple anti-inflammatory drugs and fluoroquinolones in human plasma and urine

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