Synthesis and biological evaluation of 12 novel (-)-camphene-based 1,3,4-thiadiazoles against Mycobacterium tuberculosis.

Future Microbiology
Giovana F CostacurtaRegiane B de L Scodro

Abstract

Aim: To evaluate the activity, cytotoxicity and efflux pumps inhibition of a series of 12 novels (-)-camphene-based 1,3,4-thiadiazoles (TDZs) against Mycobacterium tuberculosis (Mtb). Materials & methods: The minimum inhibitory concentration (MIC), cytotoxicity for three cell lines, ethidium bromide accumulation and checkerboard methods were carried out. Results: Compounds (6a, 6b, 6c, 6g, 6h and 6j) showed significant anti-Mtb activity (MIC 3.9-7.8 μg/ml) and no antagonism with anti-TB drugs already used in the TB treatment. Selectivity index (SI) was also determined, with values reaching 42.9 for H37Rv strain and 97.1 for clinical isolate. Five compounds also showed bacterial efflux pumps inhibition and one showed modulator effect with three drugs. Conclusion: These six TDZs should be considered as new scaffolds to develop anti-TB drugs.

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Citations

Dec 9, 2020·Journal of Biomolecular Structure & Dynamics·Md Oliullah RafiMd Shahedur Rahman
Apr 30, 2021·Microbial Drug Resistance : MDR : Mechanisms, Epidemiology, and Disease·Eloísa Gibin SampironRegiane Bertin de Lima Scodro
May 31, 2021·Trends in Microbiology·Mark LawsKhondaker Miraz Rahman

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Methods Mentioned

BETA
nuclear magnetic resonance
column chromatography
NMR

Software Mentioned

OSIRIS Property Explorer
Swiss ADME
Xcalibur

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