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Symmetrical and unsymmetrical analogues of the antimycobacterial agent isoxyl have been synthesized and tested against Mycobacterium tuberculosis H37Rv and Mycobacterium bovis BCG, some showing an increased bactericidal effect. In particular, compounds 1-(p-n-butylphenyl)-3-(4-propoxy-phenyl) thiourea (10) and 1-(p-n-butylphenyl)-3-(4-n-butoxy-phenyl) thiourea (11) showed an approximate 10-fold increase in in vitro potency compared to isoxyl, paralleled by increased inhibition of mycolic acid biosynthesis in M. bovis BCG. Interestingly, these isoxyl analogues showed relatively poor inhibition of oleate production, suggesting that the modifications have changed the spectrum of biological activity.
|Number of pages||5|
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Publication status||Published - 15 Sept 2006|
- Mycobacterium bovis
- mycolic acids
- Mycobacterium tuberculosis
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- 1 Finished
The molecular characterisation of the mode of action of the anti-TB agent isoxyl
Besra, D. & Minnikin, D.
1/10/05 → 30/09/08
Project: Research Councils