Synthesis and Characterization of Pyruvate-isoniazid Analogs and Their Copper Complexes as Potential ICL Inhibitors
Currently used anti-tubercular drugs target actively growing Mycobacterium tuberculosis (Mtb) but there are no current therapies targeting persistent mycobacteria. Isocitrate lyase (ICL) is an important enzyme of the glyoxylate shunt pathway used by Mtb for sustaining intracellular infection in inflammatory macrophages under conditions of stress such as nutrient depletion and anaerobic metabolism. Since the humans do not possess this enzyme it constitutes an attractive target for selective drug design. Present work describes synthesis and structural characterization of pyruvate-isoniazid conjugates and their copper complexes with potent anti-tubercular activities against M. Tuberculosis H37Rv. © 2012 Elsevier Ltd. All rights reserved.
D. Shingnapurkar and P. Dandawate and C. Anson and A. K. Powell and Z. Afrasiabi Navan and E. Sinn and S. Pandit and K. Venkateswara Swamy and S. Franzblau and S. Padhye, "Synthesis and Characterization of Pyruvate-isoniazid Analogs and Their Copper Complexes as Potential ICL Inhibitors," Bioorganic and Medicinal Chemistry Letters, vol. 22, no. 9, pp. 3172-3176, Elsevier, Jan 2012.
The definitive version is available at http://dx.doi.org/10.1016/j.bmcl.2012.03.047
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© 2012 Elsevier, All rights reserved.