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- W4385684325 abstract "Background: Molecular hybridization and isostery are proven approaches in medicinal chemistry, and as such we used them to design novel compounds that we investigated as potential antimycobacterials to combat drug-resistant strains. Methods & results: Prepared N-alkyl-2-(pyrimidine-5-carbonyl)hydrazine-1-carboxamides were cyclized to N-alkyl-5-(pyrimidin-5-yl)-1,3,4-oxadiazol-2-amines along with their analogues. A total of 48 compounds were tested against Mycobacterium tuberculosis H 37 Rv, Mycobacterium avium and Mycobacterium kansasii, with oxadiazoles and C 8 –C 12 alkyls being the most effective from a concentration of 2 μM. Multidrug-resistant strains were inhibited at same concentrations as the susceptible strain. For the most potent N-dodecyl-5-(pyrimidin-5-yl)-1,3,4-oxadiazol-2-amine, the mechanism of action related to cell wall biosynthesis was investigated. Conclusion: Pyrimidine-1,3,4-oxadiazole hybrids are unique antimycobacterial agents inhibiting mainly M. tuberculosis strains without cross-resistance to current drugs and are thus promising drug candidates." @default.
- W4385684325 created "2023-08-10" @default.
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- W4385684325 date "2023-06-01" @default.
- W4385684325 modified "2023-10-18" @default.
- W4385684325 title "Novel pyrimidine-1,3,4-oxadiazole hybrids and their precursors as potential antimycobacterial agents" @default.
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- W4385684325 doi "https://doi.org/10.4155/fmc-2023-0096" @default.
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