BTZ043 Racemate - CAS 957217-65-1
Catalog number: 957217-65-1
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
BTZ043 racemate is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor acting as a new antimycobacterial agent that kill Mycobacterium tuberculosis.
BTZ043 Racemate; BTZ 043 Racemate; BTZ-043 Racemate
Canonical SMILES:
1.Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.
Peng CT;Gao C;Wang NY;You XY;Zhang LD;Zhu YX;Xv Y;Zuo WQ;Ran K;Deng HX;Lei Q;Xiao KJ;Yu LT Bioorg Med Chem Lett. 2015 Apr 1;25(7):1373-6. doi: 10.1016/j.bmcl.2015.02.061. Epub 2015 Mar 2.
Tuberculosis (TB) remains a major human health problem. New therapeutic antitubercular agents are urgent needed to control the global tuberculosis pandemic. We synthesized a new series of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives and evaluated their anti-mycobacterial activities against Mycobacterium tuberculosis H37Ra as well as their druggabilities. The results showed that most of these derivatives, especially the compounds with simple alkyl side chains, exhibited good antitubercular activities and favorable aqueous solubilities with no obvious cytotoxicity. It suggested that the 4-carbonyl piperazine substituents in benzothiazinone scaffold were well tolerated, in which the compound 8h, with an antitubercular activity of MIC 0.008 μM, exhibited an excellent aqueous solubility of 104 μg/mL, which was 100-fold better than the potent DprE1 inhibitor Comp.1 (BTZ038), also more soluble than PBTZ169.
2.Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents.
Gao C;Ye TH;Wang NY;Zeng XX;Zhang LD;Xiong Y;You XY;Xia Y;Xu Y;Peng CT;Zuo WQ;Wei Y;Yu LT Bioorg Med Chem Lett. 2013 Sep 1;23(17):4919-22. doi: 10.1016/j.bmcl.2013.06.069. Epub 2013 Jul 4.
N-Alkyl and heterocycle substituted 1,3-benzothiazin-4-one (BTZ) derivatives were synthesized. The anti-mycobacterial activities of these compounds were evaluated by determination of minimal inhibitory concentration (MIC) for Mycobacterium tuberculosis H37Ra and M. tuberculosis H37Rv. It was found that an extended or branched alkyl chain analog could enhance the potency, and activities of N-alkyl substituted BTZs were not affected by either nitro or trifluoromethyl at 6-position. Trifluoromethyl plays an important role in maintaining anti-tubercular activity in the piperazine or piperidine analogs. Compound 8o, which contains an azaspirodithiolane group, showed a MIC of 0.0001 μM against M. tuberculosis H37Rv, 20-fold more potent than BTZ043 racemate. These results suggested that the volume and lipophilicity of the substituents were important in maintaining activity. In addition, compound 8o was nontoxic to Vero cells and orally bioavailable in a preliminary pharmacokinetics study.
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CAS 957217-65-1 BTZ043 Racemate

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