Sandeep Kumar Marvadi, V. Krishna, D. Sriram
Feb 15, 2019
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0
Influential Citations
22
Citations
Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
A series of novel substituted 1,2,3-triazolyldihydroquinolines 6a-o was designed and synthesized from 2-acetylthiophene in five-step reaction sequence involving modified Boltzmann-Rahtz reaction of β-Enaminone; Vilsmeier-Haack chloroformylation using DMF/POCl3; Ohira-Bestmann homologation of aldehyde to alkyne as key steps. The reaction of alkyne 4 with various aryl azides in the presence of copper sulfate and sodium ascorbate resulted desired new 1,2,3-triazolyldihydroquinolines 6a-o in excellent yields. In vitro screening of new compounds for anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv (Mtb), resulted in three derivatives 6a (MIC:1.56 µg/mL) and 6d, 6l (MIC:3.12 µg/mL) as promising antitubercular agents with lower cytotoxicity profiles.