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

2022Journal article Open access
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dc.contributor.authorGupta, Ria
dc.contributor.authorSharma, Sumit
dc.contributor.authorSingh, Rohit
dc.contributor.authorVishwakarma, Ram A.
dc.contributor.authorMignani, Serge
dc.contributor.authorSingh, Parvinder Pal
dc.date.accessioned2024-03-01T12:06:02Z
dc.date.available2024-03-01T12:06:02Z
dc.date.issued2022
dc.description.abstractNitroimidazole 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.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.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/ ph15050561pt_PT
dc.identifier.doi10.3390/ph15050561pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.13/5596
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.relationMadeira Chemistry Research Centre
dc.relationMadeira Chemistry Research Centre
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectNitroimidazolept_PT
dc.subjectSynthesispt_PT
dc.subjectAntibioticpt_PT
dc.subjectClinical usept_PT
dc.subject.pt_PT
dc.subjectFaculdade de Ciências Exatas e da Engenhariapt_PT
dc.titleFunctionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overviewpt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardTitleMadeira Chemistry Research Centre
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00674%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F00674%2F2020/PT
oaire.citation.issue5pt_PT
oaire.citation.startPage561pt_PT
oaire.citation.titlePharmaceuticalspt_PT
oaire.citation.volume15pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNameSINGH
person.familyNameMignani
person.givenNameROHIT
person.givenNameSerge
person.identifier.ciencia-id8018-B5D2-6983
person.identifier.orcid0000-0002-4235-8436
person.identifier.orcid0000-0002-1383-5256
person.identifier.ridGXG-0710-2022
person.identifier.scopus-author-id57441693900
person.identifier.scopus-author-id7003374430
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublicationf653d145-ac88-4bab-b1dd-1da472110341
relation.isAuthorOfPublicationcabd0aa0-5827-4e97-889b-922136d2dd4b
relation.isAuthorOfPublication.latestForDiscoveryf653d145-ac88-4bab-b1dd-1da472110341
relation.isProjectOfPublicatione30e13d9-be9a-4f34-91ea-a1682abce74e
relation.isProjectOfPublicatione64ad36a-83b5-467c-bbb3-449ffc0662f2
relation.isProjectOfPublication.latestForDiscoverye30e13d9-be9a-4f34-91ea-a1682abce74e

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