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Novel 1,4-substituted-1,2,3-triazoles as antitubercular agents.
journal contribution
posted on 2023-10-26, 03:22 authored by Jarrad Altimari, Samantha Hockey, H I Boshoff, A Sajid, Luke HendersonLuke HendersonTuberculosis (TB) remains a pressing unmet medical need, particularly with the emergence of multidrug-resistant and extensively drug-resistant tuberculosis. Here, a series of 1,4-substituted-1,2,3-triazoles have been synthesized and evaluated as potential antitubercular agents. These compounds were assembled via click chemistry in high crude purity and in moderate to high yield. Of the compounds tested, 12 compounds showed promising antitubercular activity with six possessing minimum inhibitory concentration (MIC) values <10 μg mL(-1) , and total selectivity for Mycobacterium tuberculosis (Mtb) growth inhibition. A second set of 21 compounds bearing variations on ring C were synthesized and evaluated. This second library gave an additional six compounds displaying MIC values ≤10 μg mL(-1) and total selectivity for Mtb growth inhibition. These compounds serve as an excellent starting point for further development of antitubercular therapies.
History
Journal
ChemMedChemVolume
10Pagination
787 - 791Location
GermanyPublisher DOI
ISSN
1860-7187eISSN
1860-7187Language
engPublication classification
C Journal article; C1 Refereed article in a scholarly journalCopyright notice
2015, Wiley-VCH VerlagUsage metrics
Keywords
Mycobacterium tuberculosisantibacterial agentsazidesclick chemistrytriazolestuberculosisScience & TechnologyLife Sciences & BiomedicineChemistry, MedicinalPharmacology & PharmacyPOTENT INHIBITORSMYCOBACTERIUM-TUBERCULOSISBIOLOGICAL EVALUATIONTRIAZOLE DERIVATIVESDRUG DEVELOPMENTDESIGNINHAOrganic Chemistry
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