950725-15-2Relevant articles and documents
Fluorinated 1,3-benzothiazin-4-ones containing fluoroquinolone fragment
Nosova, Emiliya V.,Batanova, Olga A.,Mochulskaya, Nataliya N.,Charushin, Valery N.
, (2019)
[Figure not available: see fulltext.] We have developed an efficient synthetic approach to potential antibacterial agents with double mechanism of action through the combination of antibacterial fluoroquinolones with 1,3-benzothiazin-4-ones.
Synthesis of Fluorine-Containing 2-Pyrrolyl- and 2-Indolyl-Substituted 1,3-Benzothiazin-4-ones
Nosova,Poteeva,Lipunova,Slepukhin,Charushin
, p. 384 - 387 (2019)
New 2-(1-methyl-1H-pyrrol-2-yl)- and 2-(1-methyl-1H-indol-3-yl)-5-fluoro- and -6,7,8-trifluoro-1,3-benzothiazin-4-ones have been synthesized in high yields by reaction of o-fluorobenzoyl isothiocyanates with C-nucleophilic 1-methyl-1H-pyrrole and 1-methyl
SYNTHESIS AND ANTITUBERCULAR EVALUATION OF FLUORINATED 2-CYCLOALKYLIMINO SUBSTITUTED 1,3-BENZOTHIAZIN-4-ONES
Nosova, Emiliya V.,Batanova, Olga A.,Lipunova, Galina N.,Kotovskaya, Svetlana K.,Slepukhin, Pavel A.,Kravchenko, Marionella A.,Charushin, Valery N.
, p. 69 - 77 (2019)
Novel fluorinated 2-substituted 1,3-benzothiazin-4-ones were obtained through the addition of N-nucleophiles to ortho-fluorobenzoylisothiocyanates, followed by cyclization of fluorobenzoyl-thioureas. Synthetic approaches to original 2-cycloalkylimino- and 2-carbonylpiperazino- substituted benzothiazinones, bearing different number of fluorine atoms in the benzene ring have been found. 2-Ethoxycarbonylpiperazino-5-fluoro-1,3-benzothiazin-4-one proved to exhibit a high tuberculostatic activity in vitro (MIC 0.7 microgram/mL), thus indicating that a search of biologically active compounds in this family of heterocycles appears to be a reasonable approach.
Convenient Synthesis of Fluorine-Containing 2-Aryl-5H-[1,3,4]thiadiazolo[3,2-a]quinazolin-5-ones
Nosova,Poteeva,Slepukhin
, p. 83 - 86 (2019/04/27)
An efficient synthetic approach to new fluorine-containing [1,3,4]thiadiazolo[3,2-a]quinazolin-5-ones has been developed on the basis of intramolecular cyclization of N-(N′-benzoylhydrazinecarbothioyl)-benzamides obtained from tetrafluorobenzoyl isothiocy
BENZOTHIAZINETHIONE DERIVATIVES AND THEIR PREPARATIVE METHODS AND USES
-
Paragraph 0036; 0037, (2014/05/07)
The invention belongs to the medicine field, and particularly relates to benzothiazinethione derivatives and preparation methods and uses thereof. In the aspect of the present invention, novel benzothiazinethione derivatives of formula I are provided, the benzothiazinethione derivatives of the invention are new compounds obtained based on extensive screening. Experimental results show that the benzothiazinethione derivatives of formula I have obvious inhibitory effects on mycobacterium tuberculosis, with effects equivalent to or even better than that of isoniazide (MIC90=0.8μM). The benzothiazinethione derivatives of formula I have anti-mycobacterium tuberculosis activities, and provide new choices for the development and application of antitubercular agents.
Synthesis, biological evaluation and docking study of 3-aroyl-1-(4- sulfamoylphenyl)thiourea derivatives as 15-lipoxygenase inhibitors
Mahdavi, Mohammad,Shirazi, Maryam Shahzad,Taherkhani, Raana,Saeedi, Mina,Alipour, Eskandar,Moghadam, Farshad Homayouni,Moradi, Alireza,Nadri, Hamid,Emami, Saeed,Firoozpour, Loghman,Shafiee, Abbas,Foroumadi, Alireza
, p. 308 - 313 (2014/06/24)
A series of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives containing sulfonamide moiety were designed and synthesized as 15-lipoxygenase (15-LOX) inhibitors. Most synthesized compounds showed potent activity against soybean 15-LOX with IC50
BENZOTHIAZINETHIONE DERIVATIVES AND PREPARATION METHODS AND USES THEREOF
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Paragraph 0051-0054, (2014/10/16)
Benzothiazinethione derivatives of formula (I), their preparative methods and uses are provided. Benzothiazinethione derivatives of the invention have significant effect of inhibiting Mycobacterium tuberculosis.
Fluorine-containing heterocycles: XVII. (Tetrafluorobrnzoyl)thioureas in the synthesis of fluorine-containing azaheterocycles
Lipunova,Nosova,Laeva,Trashakhova,Slepukhin,Charushin
experimental part, p. 741 - 749 (2009/04/07)
Proceeding from (tetrafluorobenzoyl)thioureas fluorine-containing derivatives were synthesized of 1-aryl-2-ethylthioquinazolin-4-one, [1,3]benzothiazin-4-one, and also of thiazolidine and 1H-1,2,4-triazole.
Fluorine-containing heterocycles: XVI. Reactions of tetrafluorobenzoyl isothiocyanate with hydrazines and their derivatives
Nosovoa,Lipunova,Laeva,Sidorova,Charushin
, p. 68 - 76 (2007/10/03)
Fluorinated derivatives of 4H-1,3-benzothiazin-4-one, [1,2,4]triazolo[4,3- a]pyrimidine, [1,2,4]triazolo[3,4-b][1,3]benzazoles, and 1,5-dihydro-1,2,4- triazole-5-thione were synthesized by addition of hydrazines and their derivatives to tetrafluorobenzoyl isothiocyanate, followed by cyclization of intermediate thiosemicarbazides.
Fluorine-containing heterocycles: XV. Reactions of polyfluorobenzoyl isothiocyanates with aminoazines and aminoazoles
Nosova,Lipunova,Laeva,Charushin
, p. 1544 - 1550 (2007/10/03)
Reactions of tetra-and pentafluorobenzoyl isothiocyanates with aminoazoles and aminoazines led to the formation of fluorinated 1,3-benzothiazin-4-ones which reacted with cyclic amines in different ways. Replacement of the N=C=S fragment was observed in so
