[Et3NH][HSO4]-mediated efficient synthesis of novel xanthene derivatives and their biological evaluation |
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Institution: | 1. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;2. Department of Pharmaceutical Chemistry, Drug Exploration and Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;3. Peptide Chemistry Department, Chemical Industries Research Division, National Research, Centre, 12622 Dokki, Cairo, Egypt |
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Abstract: | A series of novel 2-chloro quinoline incorporated xanthene derivatives were synthesized by using various 2-chloro 3-formyl quinoline, dimedone and triethylammonium hydrogen sulfate Et3NH]HSO4] as a catalyst as well solvent to give good to excellent yields. All the xanthene compounds were investigated for their in vitro antimycobacterial activity against M. tuberculosis H37Ra (MTB) and M. bovis BCG strains. Among the synthesized compounds 3a, 3c, 3d, 3e, 3g, 3h and 3k were highly potent against both the strains. Most of the active compounds were non-cytotoxic against THP-1, HCT-116, A549 and MCF-7 cell lines. Most active compounds were having higher selectively index which suggested that these compound were highly potent. |
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Keywords: | 2-Chloro quinoline Xanthene analogues Anti-tubercular activity Cytotoxicity Acidic ionic liquid |
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