PBTZ169 - CAS 1377239-83-2
Catalog number: 1377239-83-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
PBTZ169 is a decaprenyl-phosphoribose-epimerase (DprE1) inhibitor. DprE1 is an essential enzyme involved in the cell wall biosynthesis of Corynebacterineae. The MIC values of PBTZ169 ranged from 0.03 μg/mL to 0.0037 μg/mL. The MIC50 value of PBTZ169 was 0.0075μg/mL; MIC90 value was 0.030 μg/mL.
PBTZ169; PBTZ-169; PBTZ 169; macozinone; 2-(4-(cyclohexylmethyl)piperazin-1-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one
DMSO ≥ 6.4 mg/mL
-20°C Freezer
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
1.Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.
Lv K;Tao Z;Liu Q;Yang L;Wang B;Wu S;Wang A;Huang M;Liu M;Lu Y Eur J Med Chem. 2018 May 10;151:1-8. doi: 10.1016/j.ejmech.2018.03.060. Epub 2018 Mar 23.
We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC < 1 μg/mL) against drug-susceptible Mycobacterium tuberculosis H37RV strain. After two set of modifications, compound 2i were found to display comparable in vitro anti-TB activity (MIC < 0.016 μg/mL) to PBTZ169 against drug-sensitive and resistant mycobacterium tuberculosis strains. Compound 2i also showed acceptable PK profiles. Studies to determine PK profiles in lung and in vivo efficacy of 2i are currently under way.
2.Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis.
Lechartier B;Cole ST Antimicrob Agents Chemother. 2015 Aug;59(8):4457-63. doi: 10.1128/AAC.00395-15. Epub 2015 May 18.
Clofazimine (CZM) is an antileprosy drug that was recently repurposed for treatment of multidrug-resistant tuberculosis. In Mycobacterium tuberculosis, CZM appears to act as a prodrug, which is reduced by NADH dehydrogenase (NDH-2), to release reactive oxygen species upon reoxidation by O2. CZM presumably competes with menaquinone (MK-4), a key cofactor in the mycobacterial electron transfer chain, for its reduction by NDH-2. We studied the effect of MK-4 supplementation on the activity of CZM against M. tuberculosis and found direct competition between CZM and MK-4 for the cidal effect of CZM, against nonreplicating and actively growing bacteria, as MK-4 supplementation blocked the drug's activity against nonreplicating bacteria. We demonstrated that CZM, like bedaquiline, is synergistic in vitro with benzothiazinones such as 2-piperazino-benzothiazinone 169 (PBTZ169), and this synergy also occurs against nonreplicating bacteria. The synergy between CZM and PBTZ169 was lost in an MK-4-rich medium, indicating that MK-4 is the probable link between their activities. The efficacy of the dual combination of CZM and PBTZ169 was tested in vivo, where a great reduction in bacterial load was obtained in a murine model of chronic tuberculosis.
3.Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
Tiwari R;Miller PA;Chiarelli LR;Mori G;Šarkan M;Centárová I;Cho S;Mikušová K;Franzblau SG;Oliver AG;Miller MJ ACS Med Chem Lett. 2016 Jan 4;7(3):266-70. doi: 10.1021/acsmedchemlett.5b00424. eCollection 2016 Mar 10.
Electron deficient nitroaromatic compounds such as BTZ043 and its closest congener, PBTZ169, and related agents are a promising new class of anti-TB compounds. Herein we report the design and syntheses of 1,3-benzothiazinone azide (BTZ-N3) and related click chemistry products based on the molecular mode of activation of BTZ043. Our computational docking studies indicate that BTZ-N3 binds in the essentially same pocket as that of BTZ043. Detailed biochemical studies with cell envelope enzyme fractions of Mycobacterium smegmatis combined with our model biochemical reactivity studies with nucleophiles indicated that, in contrast to BTZ043, the azide analogue may have a different mode of activation for anti-TB activity. Subsequent enzymatic studies with recombinant DprE1 from Mtb followed by MIC determination in NTB1 strain of Mtb (harboring Cys387Ser mutation in DprE1 and is BTZ043 resistant) unequivocally indicated that BTZ-N3 is an effective reversible and noncovalent inhibitor of DprE1.
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