Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098: An attempt to improve the activity against Mycobacterium tuberculosis
2011 (English)In: Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, E-ISSN 1090-2120, Vol. 21, no 18, 5403-5407 p.Article in journal (Refereed) Published
Two series of FR900098/fosmidomycin analogs were synthesized and evaluated for MtDXR inhibition and Mycobacterium tuberculosis whole-cell activity. The design rationale of these compounds involved the exchange of either the phosphonic acid or the hydroxamic acid part for alternative acidic and metal-coordinating functionalities. The best inhibitors provided IC(50) values in the micromolar range, with a best value of 41 mu M.
Place, publisher, year, edition, pages
2011. Vol. 21, no 18, 5403-5407 p.
Tuberculosis, DXR, Enzyme inhibitor, Fosmidomycin, FR900098
IdentifiersURN: urn:nbn:se:uu:diva-158288DOI: 10.1016/j.bmcl.2011.07.005ISI: 000294051800057OAI: oai:DiVA.org:uu-158288DiVA: diva2:439403