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957217-65-1

BTZ043 (BTZ038, BTZ044) is a chemical with a specific purpose. Lookchem provides you with multiple data and supplier information of this chemical.

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  • 957217-65-1 Structure

  • Basic information

    1. Product Name: BTZ043 (BTZ038, BTZ044)
    2. Synonyms: BTZ043 (BTZ038, BTZ044);4H-1,3-Benzothiazin-4-one, 2-(2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-8-nitro-6-(trifluoromethyl)-;2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one BTZ043 Racemate;Benzothiazinone 10526038;BTZ 10526038;2-(2-Methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one
    3. CAS NO:957217-65-1
    4. Molecular Formula: C17H16F3N3O5S
    5. Molecular Weight: 431.3862496
    6. EINECS: 604-604-1
    7. Product Categories: Inhibitors
    8. Mol File: 957217-65-1.mol

  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: 547.6±60.0 °C(Predicted)
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: 1.68±0.1 g/cm3(Predicted)
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: insoluble in H2O; ≥10.4 mg/mL in DMSO with gentle warming; ≥3.27 mg/mL in EtOH with gentle warming and ultrasonic
    9. PKA: -0.51±0.20(Predicted)
    10. CAS DataBase Reference: BTZ043 (BTZ038, BTZ044)(CAS DataBase Reference)
    11. NIST Chemistry Reference: BTZ043 (BTZ038, BTZ044)(957217-65-1)
    12. EPA Substance Registry System: BTZ043 (BTZ038, BTZ044)(957217-65-1)

  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 957217-65-1(Hazardous Substances Data)

957217-65-1 Usage

Biological Activity

mic: 1 ng/ml (2.3 nm) for m. tuberculosis h37rv and 4 ng/ml (9.2 nm) for mycobacterium smegmatisthe loss of human lives to tuberculosis (tb) continues unabated as a result of poverty, synergy with the hiv/aids pandemic, and the emergence of multidrug- and extensively drug-resistant strains of mycobacterium tuberculosis. btz043 is the most advanced candidate for inclusion in combination therapies for both drug-sensitive and extensively drug-resistant tb.

in vitro

btz043 displayed similar activity against all clinical isolates of m. tuberculosis that were tested, including extensively drug-resistant and multidrug-resistant strains, indicating that it targets a previously unknown biological function. btz043 is bactericidal, reducing viability in vitro by more than 1000-fold in under 72 hours, which is comparable to the inh killing effect [1].

in vivo

the in vivo efficacy of btz043 was assessed 4 weeks after a low-dose aerosol infection of in the chronic balb/c mice model of tb. four weeks of treatment with btz043 reduced the bacterial load in the lungs and spleens by 1 and 2 logs, respectively, at the concentrations used. additional findings suggest that btz efficacy is time- rather than dose-dependent [1].

references

[1] makarov v, manina g, mikusova k, et al. benzothiazinones kill mycobacterium tuberculosis by blocking arabinan synthesis. science. 2009 may 8;324(5928):801-4.

Check Digit Verification of cas no

The CAS Registry Mumber 957217-65-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,5,7,2,1 and 7 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 957217-65:
(8*9)+(7*5)+(6*7)+(5*2)+(4*1)+(3*7)+(2*6)+(1*5)=201
201 % 10 = 1
So 957217-65-1 is a valid CAS Registry Number.

957217-65-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 20, 2017

Revision Date: Aug 20, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-(3-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-one

1.2 Other means of identification

Product number -
Other names BTZ038

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:957217-65-1 SDS

957217-65-1Downstream Products

957217-65-1Relevant articles and documents

Efficient Synthesis of Benzothiazinone Analogues with Activity against Intracellular Mycobacterium tuberculosis

Richter, Adrian,Narula, Gagandeep,Rudolph, Ines,Seidel, Rüdiger W.,Wagner, Christoph,Av-Gay, Yossef,Imming, Peter

, (2021/12/27)

8-Nitrobenzothiazinones (BTZs) are a promising class of antimycobacterial agents currently under investigation in clinical trials. Starting from thiourea derivatives, a new synthetic pathway to BTZs was established. It allows the formation of the thiazinone ring system in one synthetic step and is applicable for preparation of a wide variety of BTZ analogues. The synthetic procedure furthermore facilitates the replacement of the sulphur atom in the thiazinone ring system by oxygen or nitrogen to afford the analogous benzoxazinone and quinazolinone systems. 36 BTZ analogues were prepared and tested in luminescence-based assays for in vitro activity against Mycobacterium tuberculosis (Mtb) using the microdilution broth method and a high-throughput macrophage infection assay.

Synthesis and structure-activity relationships evaluation of benzothiazinone derivatives as potential anti-tubercular agents

Gao, Chao,Ye, Ting-Hong,Wang, Ning-Yu,Zeng, Xiu-Xiu,Zhang, Li-Dan,Xiong, Ying,You, Xin-Yu,Xia, Yong,Xu, Ying,Peng, Cui-Ting,Zuo, Wei-Qiong,Wei, Yuquan,Yu, Luo-Ting

, p. 4919 - 4922 (2013/09/02)

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 H3

Identification of antitubercular benzothiazinone compounds by ligand-based design

Karoli, Tomislav,Becker, Bernd,Zuegg, Johannes,M?llmann, Ute,Ramu, Soumya,Huang, Johnny X.,Cooper, Matthew A.

, p. 7940 - 7944 (2012/10/29)

1,3-Benzothiazin-4-ones (BTZs) are a novel class of TB drug candidates with potent activity against M. tuberculosis. An in silico ligand-based model based on structure-activity data from 170 BTZ compounds was used to design a new series. Compounds were tested against a panel of mycobacterial strains and were profiled for cytotoxicity, stability, and antiproliferative effects. Several of the compounds showed improved activity against MDR-TB while retaining low toxicity with higher microsomal, metabolic, and plasma stability.

Process for the preparation of 2-aminosubstituted 1,3-benzothiazine-4-ones

-

Page/Page column 11, (2011/11/07)

A process for preparing 2-aminosubstituted 1,3-benzothiazine-4-ones is provided which comprises the following step: wherein Y is halogen; R is independently selected from C1-6-alkyl which may optionally be substituted by halogen, -NO2, halogen, -CHO -COOR4 (wherein R4 is hydrogen or C1-6-alkyl) and -CN; R3 is C1-3-alkyl which may be substituted by halogen; X is halogen; and n is 0 or an integer of 1 to 4; if n is 2, 3 or 4, multiple Rs may be the same or different.

PROCESS FOR THE PREPARATION OF 2-AMINO-SUBSTITUTED 1,3-BENZOTHIAZINE-4-ONES

-

Page/Page column 19, (2011/11/06)

A process for preparing 2-aminosubstituted 1, 3 -benzothiazine- 4 -ones is provided which comprises the following step: Formula (I) wherein Y is halogen; R is independently selected from C1-6-alkyl which may optionally be substituted by halogen, -NO2, halogen, -CHO -COOR4 (wherein R4 is hydrogen or C1-6-alkyl) and -CN; R3 is C1-6-alkyl which may be substituted by halogen; X is halogen; and n is 0 or an integer of 1 to 4; if n is 2, 3 or 4, multiple Rs may be the same or different.

Benzothiazinone Derivatives and their Use as Antibacterial Agents

-

Page/Page column 3, (2009/10/01)

The present invention relates to novel benzothiazin derivatives and their use as antibacterial agents in infectious diseases of mammals (humans and animals) caused by bacteria, especially diseases like tuberculosis (TB) and leprosy caused by mycobacteria.

NEW BENZOTHIAZINONE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS

-

Page/Page column 9, (2008/06/13)

Novel benzothiazin derivatives of formula (I) and their use as antibacterial agents in infectious diseases caused by bacteria, especially tuberculosis (TB) and leprosy caused by mycobacteria, wherein R1 and R2are, independently each

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