Synonyms: PBTZ169
Compound class:
Synthetic organic
Comment: Macozinone (PBTZ169) is the lead from a series of piperazine-containing benzothiazinones [1]. It has potent antimycobacterial activity and is under clinical evaluation as a treatment for tuberculosis (TB). Macozinone is an inhibitor of decaprenylphosphoryl-beta-D-ribose oxidase (DprE1), an essential mycobacterial cell wall biosynthesis enzyme [1].
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Bioactivity Comments |
The MIC99 for in vitro activity against Mycobacterium tuberculosis H37Rv is 0.3 ng/ml and macozinone is three- to seven-fold more active than BTZ-043 when tested against a panel of Actinobacteria [1]. Macozinone has been shown to have synergistic activity when combined with telacebec (Q203) [2]. |