Vývoj nové skupiny potenciálních antituberkulotik
Development of new group of potential antituberculotics
rigorous thesis (DEFENDED)
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http://hdl.handle.net/20.500.11956/14246Identifiers
Study Information System: 53345
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- Kvalifikační práce [6562]
Author
Advisor
Referee
Kolář, Karel
Faculty / Institute
Faculty of Pharmacy in Hradec Králové
Discipline
Pharmacy
Department
Department of Inorganic And Organic Chemistry
Date of defense
5. 2. 2008
Publisher
Univerzita Karlova, Farmaceutická fakulta v Hradci KrálovéLanguage
Czech
Grade
Pass
In this rigorous paper three problems were solved: a) synthesis and antimycobacterial activity of new halogenated salicylanilides substituted in position 4' with branch chain. b) synthesis and antimycobacterial activity of new halogenated 3-(4-alkylphenyl)-1,3-benzoxazine-2,4-(3H)-diones. c) influence of replacement of oxo group by thioxo group in the previously group of compounds. a) It was synthesized 8 halogenated derivatives of 4'-alkylsalicylanilides with branched alkyl chain. These compounds were evaluated in vitro on antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium. b) It was synthesized 7 halogenated derivatives of benzoxazinediones with branch chain by reaction of salicylanilides with methylchloroformiate. Antimycobacterial activity of synthesized compounds was evaluated against three different mycobacterial strains. The most active compound was 7- chloro-3-(4-sec-butylphenyl)-1,3-benzoxazine-2,4-(3H)-dione. c) There were synthesized the following compounds: 7-chloro-3-(4-isopropylphenyl)-4-thioxo-2H-1,3- benzoxazine-2(3H)-one, 6-bromo-3-(4-isopropylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-one, 6- bromo-3-(4-sec-butylphenyl)-4-thioxo-2H-1,3-benzoxazine-2(3H)-one, 6-chloro-3-(4-sec-...