58779-09-2Relevant academic research and scientific papers
SYNTHESIS OF INHIBITORS OF FTSZ
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Page/Page column 76-77, (2008/06/13)
FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2"'-hydroxy-5"-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.
Synthesis of antimicrobial natural products targeting FtsZ: (±)-dichamanetin and (±)-2?-hydroxy-5″- benzylisouvarinol-B
Urgaonkar, Sameer,La Pierre, Henry S.,Meir, Israel,Lund, Henrik,RayChaudhuri, Debabrata,Shaw, Jared T.
, p. 5609 - 5612 (2007/10/03)
(Chemical Equation Presented) Two natural products have been synthesized using a ZnCl2-mediated benzylic coupling reaction. Both are potent inhibitors of the GTPase activity of FtsZ, a highly conserved protein that is essential for bacterial cytokinesis.
