Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098 : An attempt to improve the activity against Mycobacterium tuberculosis

• 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.

Ämnesord

NATURVETENSKAP  -- Kemi (hsv//swe)

NATURAL SCIENCES  -- Chemical Sciences (hsv//eng)

Nyckelord

Tuberculosis

DXR

Enzyme inhibitor

Fosmidomycin

FR900098

Chemistry

Kemi

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