22227-47-0

Upstream product

• 22227-59-4 2-chloro-3-nitro-5-(trifluoromethyl)benzoic acid 
• 657-06-7 2-chloro-5-trifluoromethylbenzoic acid 
• 98-56-6 4-chlorobenzotrifluoride 
• 87033-30-5 2-chloro-3-nitro-5-(trifluoromethyl)benzoyl chloride 

Downstream Products

• 957217-76-4 2-(aminocarbonyl)-6-nitro-4-(trifluoromethyl)phenyl-1,4-dioxa-8-azaspiro[4.5]decane-8-carbodithioate 
• 1161233-85-7 2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one 
• 1377239-83-2 2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one 

Relevant academic research and scientific papers

Macozinone: Revised synthesis and crystal structure of a promising new drug for treating drug-sensitive and drug-resistant tuberculosis

Mycobacterium tuberculosis (Mtb), the principal etiological agent of tuberculosis (TB), infects over one-quarter of humanity and is now the leading cause of infectious disease mortality by a single pathogen. Macozinone {2-[4-(cyclohexylmethyl)piperazin-1-

Design, synthesis and antitubercular evaluation of benzothiazinones containing an oximido or amino nitrogen heterocycle moiety

A series of 8-nitro-6-(trifluoromethyl)-1,3-benzothiazin-4-ones (BTZs) bearing an oximido or amino nitrogen heterocycle moiety through modifications at the C-2 position of BTZ043 and BPTZ169 were designed and synthesized as new antitubercular agents. Many of the target compounds demonstrate excellent in vitro activity (MIC: ?1) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosis (MTB) strains. Compound 10a displays acceptable safety, aqueous solubility and pharmacokinetic properties, opening up a new possibility for further development.

BENZOTHIAZINONE DERIVATIVES AS ANTI -TUBERCULOSIS AGENTS

Novel benzothiazinone derivatives of formula (I) or pharmaceutically acceptable salts or solvates thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis: wherein EWG (electron withdrawing group) = NO2, CN, CF3, F, Cl, Br, OCF3, OH, OR, OCHF2, COOR, wherein R is hydrogen or a straight or branched C1-C4 alkyl group, X = a bond or a straight or branched C1-C4 alkylene group which may be substituted with a group selected from F, Cl, Br, I or C1-C4 alkoxy; Y = hydrogen, a straight or branched C1-C4 alkyl group, OH or OR, wherein R is hydrogen or a straight or branched C1-C4 alkyl group; n = 0, 1 or 2; R1, R2 = hydrogen or substituent (s) which may be the same or different from each other and are selected from the group consisting of D, F, Cl, Br, CF3, a straight or branched C1-C4 alkyl group, a phenyl group, OR, SR, NR3R4, wherein R, R3, R4 may be the same or different from each other and are hydrogen or a straight or branched C1-C4 alkyl group or a phenyl group.

Benzothiazinone compounds and their use as anti-tuberculosis agents

Novel benzothiazinone derivatives of formula (I) or a pharmaceutically acceptable salt or solvate thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis

NOVEL ANTI-TUBERCULOSIS AGENTS

Novel benzothiazinone derivatives of formula (I) or a pharmaceutically acceptable salt or solvate thereof have been found to be effective against Mycobacterium tuberculosis strains and may thus be useful in the treatment of tuberculosis (I) wherein, EWG (electron withdrawing group) = N02, CN, CF3, F, CI, Br, OCF3, OH, OR, OCHF2, COOR, wherein R is hydrogen, or a straight or branched C1-C4 alkyl group, X = a bond, or a straight or branched C1-C4 alkylene group; Y = a bond, or a straight or branched C1-C4 alkylene group; wherein either one of X or Y is a bond and the other is a Ci-C4-alkylene group, Z = N or C, n = 1 or 2; R1 = hydrogen, a straight or branched C1-C6 alkyl group, or a C3-C6 cycloalkyl group, which may be substituted with a group selected from F, CI, Br, I or a C1-C4 alkoxy; R2 = a phenyl group, a naphthyl group or a thienyl group, each of which may be unsubstituted or substituted with one or more substituent(s) which may be the same or different from each other, selected from the group consisting of F, CI, Br, I, CN, NO2, or a straight or branched C1-C6 alkyl or phenyl group, which may be substituted with a group selected from F, CI, Br, I, or C1-C4 alkoxy.

Benzothiazinone Derivatives and their Use as Antibacterial Agents

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

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

Substituted diphenyl ethers

A compound of the formula: STR1 and salts and esters thereof, useful as intermediates for the preparation of compounds of the formula STR2 wherein R1 is an alkyl group optionally substituted by one or more fluorine atoms or by an optionally substituted phenyl group R2 is No2 or Cl and R6 is a hydrogen atom or an alkyl group of 1 to 4 carbon atoms.