Synthesis and evaluation of isosteres of N-methyl indolo [3, 2-b]-quinoline (cryptolepine) as new antiinfective agents

…, S Li, A Khan, W Zhang, P Fan, M Jacob, S Khan…

文献索引：Zhu, Xue Y.; Mardenborough, Leroy G.; Li, Shouming; Khan, Abdul; Zhang, Wang; Fan, Pincheng; Jacob, Melissa; Khan, Shabana; Walker, Larry; Ablordeppey, Seth Y. Bioorganic and Medicinal Chemistry, 2007 , vol. 15, # 2 p. 686 - 695

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被引用次数: 41

摘要

Isosteres of cryptolepine (1) were synthesized and evaluated for their antiinfective activities. Overall, the sulfur isostere, 5-methyl benzothieno [3, 2-b] quinolinium salt (5b), was equipotent to 1 and has shown no cytotoxicity at 23.8 μg/mL. Compound 5b was also found to have a broad spectrum of activity. Both the carbon and oxygen isosteres were less potent than cryptolepine. A limited library of 2-substituted analogs of 5b has been synthesized ...