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Substitution of the phosphonic acid and hydroxamic acid functionalities of the DXR inhibitor FR900098 : An attempt to improve the activity against Mycobacterium tuberculosis
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- Andaloussi, Mounir (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Lindh, Martin, 1981- (author)
- Uppsala universitet,Avdelningen för organisk farmaceutisk kemi
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- Björkelid, Christofer (author)
- Uppsala universitet,Struktur- och molekylärbiologi
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- Iyer, Harini (author)
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- (creator_code:org_t)
- Elsevier BV, 2011
- 2011
- English.
- In: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 21:18, s. 5403-5407
- Journal article (peer-reviewed)
Abstract
Subject headings
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- 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.
Subject headings
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Keyword
- Tuberculosis
- DXR
- Enzyme inhibitor
- Fosmidomycin
- FR900098
- Chemistry
- Kemi
Publication and Content Type
- ref (subject category)
- art (subject category)
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