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Publication
Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview
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Advisor(s)
Abstract(s)
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.
Description
Keywords
Nitroimidazole Synthesis Antibiotic Clinical use . Faculdade de Ciências Exatas e da Engenharia
Citation
: Gupta, R.; Sharma, S.; Singh, R.; Vishwakarma, R.A.; Mignani, S.; Singh, P.P. Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview. Pharmaceuticals 2022, 15, 561. https://doi.org/10.3390/ ph15050561
Publisher
MDPI