- 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
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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 expe
- Tangallapally, Rajendra P.,Lee, Robin E.B.,Lenaerts, Anne J.M.,Lee, Richard E.
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p. 2584 - 2589
(2007/10/03)
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- HETEROCYCLIC AMIDES WITH ANTI-TUBERCULOSIS ACTIVITY
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Compounds having the general structure (I) : wherein A is selected from the group consisting of oxygen, sulfur, and NR15, and R15 is selected from the group consisting of H, alkyl, aryl, substituted alkyl, and substituted aryl; B, D, and E are each independently selected from the group consisting of CH, nitrogen, sulfur and oxygen; R1 is selected from the group consisting of nitro, halo, alkyl ester, phenylsulfanyl, phenylsulfinyl, phenylsulfonyl and sulfonic acid; t is an integer from 1 to 3; and X is a substituted amide and methods of using the novel compounds for treating infections caused microorganisms, including Mycobacterium tuberculosis.
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