Nitroimidazoles, Metronidazole, Ornidazole and Tinidazole; and Fidaxomicin

Wilcox, Mark H.

doi:10.1016/b978-0-7020-6285-8.00147-7

Cited by 6 publications

(4 citation statements)

References 24 publications

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“…Ornidazole is a nitroimidazole based drug and was selected for the study for its common use as antibiotic for treating a range of anaerobic bacterial infections. [32][33][34] Our study also reveals that it is possible to not only to highly polarise this drug but also to separate it from the heavy metal catalyst using the technique of phase extraction. The results further indicate that this and other related drugs could be potentially prepared for biomedical use in a cheap and cost-effective way by using PHIP and SABRE.…”

Section: Introductionmentioning

confidence: 75%

¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

Iali

Moustafa

Dagys

et al. 2021

Magnetic Reson in Chemistry

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Signal amplification by reversible exchange (SABRE) offers a cost-effective route to boost nuclear magnetic resonance (NMR) signal by several orders of magnitude by employing readily available para-hydrogen as a source of hyperpolarisation. Although 1 H spins have been the natural choice of SABRE hyperpolarisation since its inception due to its simplicity and accessibility, limited spin lifetimes of 1 H makes it harder to employ them in a range of timedependent NMR experiments. Heteronuclear spins, for example, 13 C and 15 N, in general have much longer T 1 lifetimes and thereby are found to be more suitable for hyperpolarised biological applications as demonstrated previously by para-hydrogen induced polarisation (PHIP) and dynamic nuclear

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Section: Introductionmentioning

confidence: 75%

¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

Iali

Moustafa

Dagys

et al. 2021

Magnetic Reson in Chemistry

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“…Ornidazole 8 (Tiberal ® ) is an antibiotic used to treat protozoan infections ( Figure 12 ). [ 101 , 109 , 110 , 111 ] It has been shown to produce successful cures in 87% of cases. It was discovered by Tiberal and Hoffmann in the year 1974 and is marketed by Roche.…”

Section: Activity Profile and Synthetic Pathways Developed To Constru...mentioning

confidence: 99%

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview

et al. 2022

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Nitroimidazole represents one of the most essential and unique scaffolds in drug discovery since its discovery in the 1950s. It was K. Maeda in Japan who reported in 1953 the first nitroimidazole as a natural product from Nocardia mesenterica with antibacterial activity, which was later identified as Azomycin 1 (2-nitroimidazole) and remained in focus until now. This natural antibiotic was the starting point for synthesizing numerous analogs and regio-isomers, leading to several life-saving drugs and clinical candidates against a number of diseases, including infections (bacterial, viral, parasitic) and cancers, as well as imaging agents in medicine/diagnosis. In the present decade, the nitroimidazole scaffold has again been given two life-saving drugs (Delamanid and Pretomanid) used to treat MDR (multi-drug resistant) tuberculosis. Keeping in view the highly successful track-record of the nitroimidazole scaffold in providing breakthrough therapeutic drugs, this comprehensive review focuses explicitly on presenting the activity profile and synthetic chemistry of functionalized nitroimidazole (2-, 4- and 5-nitroimidazoles as well as the fused nitroimidazoles) based drugs and leads published from 1950 to 2021. The present review also presents the miscellaneous examples in each class. In addition, the mutagenic profile of nitroimidazole-based drugs and leads and derivatives is also discussed.

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“…Nitroimidazole absorption is high in oral administration, with a relatively low binding rate to protein. Nitroimidazole is metabolized in the liver and excreted through urine [ 53 ].…”

Section: Progressmentioning

confidence: 99%

Recent Progress and Challenges for Drug-Resistant Tuberculosis Treatment

2021

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Control of Mycobacterium tuberculosis infection continues to be an issue, particularly in countries with a high tuberculosis (TB) burden in the tropical and sub-tropical regions. The effort to reduce the catastrophic cost of TB with the WHO’s End TB Strategy in 2035 is still obstructed by the emergence of drug-resistant TB (DR-TB) cases as result of various mutations of the MTB strain. In the approach to combat DR-TB, several potential antitubercular agents were discovered as inhibitors for various existing and novel targets. Host-directed therapy and immunotherapy also gained attention as the drug-susceptibility level of the pathogen can be reduced due to the pathogen’s evolutionary dynamics. This review is focused on the current progress and challenges in DR-TB treatment. We briefly summarized antitubercular compounds that are under development and trials for both DR-TB drug candidates and host-directed therapy. We also highlighted several problems in DR-TB diagnosis, the treatment regimen, and drug discovery that have an impact on treatment adherence and treatment failure.

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Nitroimidazoles, Metronidazole, Ornidazole and Tinidazole; and Fidaxomicin

Cited by 6 publications

References 24 publications

¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview

Recent Progress and Challenges for Drug-Resistant Tuberculosis Treatment

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Nitroimidazoles, Metronidazole, Ornidazole and Tinidazole; and Fidaxomicin

Cited by 6 publications

References 24 publications

15N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

15N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview

Recent Progress and Challenges for Drug-Resistant Tuberculosis Treatment

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Product

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¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium

¹⁵N hyperpolarisation of the antiprotozoal drug ornidazole by Signal Amplification By Reversible Exchange in aqueous medium