Design, diversity-oriented synthesis and structure activity relationship studies of quinolinyl heterocycles as antimycobacterial agents

作者：Rachakonda Venkatesham; Alla Manjula^*; Kotipalli Sudha Sravanti; Ummanni Ramesh

来源：European Journal of Medicinal Chemistry, 2013, 70: 536-547.

DOI：10.1016/j.ejmech.2013.10.034

• Tuberculosis
• Cytotoxicity
• Antimycobacterial
• Diversity oriented synthesis
• Bis heterocycles
• 3-Acyl/carboxylate-quinoline

The current study reports design and diversity oriented synthesis of novel bis heterocycles with a common 2-methyl, C-4 unsubstituted quinoline moiety as the central key heterocycle. Employing reagent based skeletal diversity approach; a facile synthesis of bis heterocycles with different heterocyclic rings at C-3 position of the quinoline moiety has been accomplished. A broad range of heterocyclic frameworks thus obtained were evaluated for their antimycobacterial activity. The active scaffolds were further explored by a parallel library generation in order to establish SAR. Further, low cytotoxicity against A549 cell line enhances the potential of the synthesized molecules as promising antimycobacterial agents.

• 出版日期2013-12