| Literature DB >> 30064024 |
Gautam Kumar1, Asawari Sathe1, Vagolu Siva Krishna2, Dharmarajan Sriram2, Sanjay M Jachak3.
Abstract
Sodium trifluoromethanesulfonate, and glacial acetic acid selectively catalyzed the synthesis of dihydroquinoline via Friedländer annulation. The synthesized dihydroquinoline analogues coupled with different amines by the use of coupling reagent gave dihydroquinoline carboxamide derivatives in moderate to good yields. All the synthesized novel compounds were evaluated for the anti-tubercular activity and cytotoxic activities in vitro. Among tested 30 compounds, two compounds, 8g and 8h showed MIC value of 0.39 and 0.78 μg/mL, respectively against Mycobacterium tuberculosis H37Rv and they were found to be non-toxic. Also these two compounds exhibited good pharmacological properties and oral absorption when studied using in-silico models.Entities:
Keywords: ADME; Anti-tubercular activity; Dihydroquinoline; Friedländer synthesis; Sodium trifluoromethanesulfonate
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Year: 2018 PMID: 30064024 DOI: 10.1016/j.ejmech.2018.07.046
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514