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• W2936024054 abstract "• New potent anti-TB spirooxindolopyrrolizidines were designed & synthesized by green methodology. • High yields of the products in less reaction time and reusability of the ionic liquid. • Dept-135 and crystallographic studies of the compound 6f . • Anti-TB activity evaluation of all compounds & identifying leads ( 6h , 6e , 6k , 6l , 6n , 6q & 6r ) as promising anti-TB agents. • 6 compounds exhibited anti-TB activity equal to drug Ethambutol and 1 compound exhibited superior activity than ethambutol. The aim of the study is to design and synthesis of a new series of potent anti-TB 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines with their safety profile. A synergetic effect of ultrasonication and ionic liquid was shown successfully as a green methodology for the synthesis of title compounds 6a–t . These derivatives were obtained in shorter reaction time with good yields and well characterized by various spectroscopic methods, single-crystal X-ray diffraction ( 6f ). The in vitro anti-tuberculosis activity for newly-synthesized derivatives has been screened against Mycobacterium tuberculosis . Among all, six compounds 6e , 6k , 6l , 6n , 6q and 6r exhibited equal potent activity compared to standard drug ethambutol (MIC: 1.56 µg/mL) and another compound 6h exhibited outstanding activity (MIC: 0.78 µg/mL) than the standard drug ethambutol. Cytotoxic nature of the anti-TB active compounds was evaluated against RAW 264.7 cells. The 6h , 6e , 6k , 6l , 6n , 6q and 6r exhibited lower toxicity which could be promising hits for anti-tuberculosis." @default.
• W2936024054 created "2019-04-25" @default.
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• W2936024054 date "2019-07-01" @default.
• W2936024054 modified "2023-10-12" @default.
• W2936024054 title "Ultrasonication-ionic liquid synergy for the synthesis of new potent anti-tuberculosis 1,2,4-triazol-1-yl-pyrazole based spirooxindolopyrrolizidines" @default.
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• W2936024054 doi "https://doi.org/10.1016/j.bmcl.2019.04.026" @default.
• W2936024054 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31047752" @default.
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