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New groups of potential antituberculotics with thioxo group
Husáková, Petra ; Waisser, Karel (advisor) ; Kolář, Karel (referee)
. ENGLISH ABSTRACT In the rigorous thesis are described the influence of replacement oxo group for thioxo group in the series of halogenated 3-(4-ethylphenyl)benzoxazine-2,4(3H)-diones and 6-chloro-3- (4-butylphenyl)benzoxazine-2,4(3H)-dione. The starting ethyl (or butyl) salicylanilides were synthesis from substituted salicylic acid and ethyl (or butyl) aniline in toluene by the presence of phosphorus trichloride. (The set of halogenated salicyl acids compounds: 4-chloro-, 5-chloro-, 5- bromo- and 3,5-dibromosalicylic acid). The halogenated 4'-ethylsalicylanilides were reacted in dry pyridine with methyl-chloroformiate to form 3-(4-ethylphenyl)benzoxazine-2,4(3H)-diones. Similar were prepared 6-chloro-3-(4-butylphenyl)benzoxazine-2,4(3H)-diones. The mixture of 3- (4-ethyphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-one and 3-(4-ethylphenyl)-2H-1,3- benzoxazine-2,4(3H)-dithione was prepared by the reaction of the halogenated 3-(4- ethylphenyl)- 2H-1,3-benzoxazine-2,4(3H)-diones with phosphorus pentasulfide. The products were separated by chromatography. The 3-(4-ethylphenyl)-6-chloro-4-thioxo-2H-1,3- benzoxazine-2(3H)-ones and 6-chloro-3-(4-ethylphenyl)-2H-1,3-benzoxazine-2,4(3H)-dithiones were prepared by similar way. The compounds were tested in vitro for antimycobacterial activity against Mycobacterium...
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