Identification of a novel class of quinoline–oxadiazole hybrids as anti-tuberculosis agents

[Display omitted] A series of novel quinoline–oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity a...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2016-01, Vol.26 (2), p.645-649
Hauptverfasser: Jain, Puneet P., Degani, Mariam S., Raju, Archana, Anantram, Aarti, Seervi, Madhav, Sathaye, Sadhana, Ray, Muktikanta, Rajan, M.G.R.
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Sprache:eng
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Zusammenfassung:[Display omitted] A series of novel quinoline–oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity against Mycobacterium tuberculosis H37Rv and for cytotoxicity in HepG2 cell line. Several of the hits exhibited good to excellent anti-tuberculosis activity and selectivity, especially compounds 12m, 12o and 12p, showed minimum inhibitory concentration values500. The results of this study open up a promising avenue that may lead to the discovery of a new class of anti-tuberculosis agents.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.11.057