Synthesis of new and potent analogues of anti-tuberculosis agent 5-nitro-furan-2-carboxylic acid 4-(4-benzyl-piperazin-1-yl)-benzylamide with improved bioavailability

RP Tangallapally, REB Lee, AJM Lenaerts…

文献索引：Tangallapally, Rajendra P.; Lee, Robin E.B.; Lenaerts, Anne J.M.; Lee, Richard E. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 10 p. 2584 - 2589

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被引用次数: 40

摘要

Previously, the lead compound 5-nitro-furan-2-carboxylic acid 4-(4-benzyl-piperazin-1-yl)- benzylamide was identified in our anti-tuberculosis drug discovery program. Although this compound demonstrated excellent in vitro activity, it did not meet the expected in vivo profiles due to structural features that resulted in rapid metabolic cleavage and poor absorption, which therefore limited its bioavailability. In efforts to increase the ...