Maxer M. Synthesis, physical, chemical and biological properties of 4-(adamantly-1)-thiazolyl-2-amine acyl derivatives

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0403U001193

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

21-03-2003

Specialized Academic Board

Д64.605.01

Essay

A preparative method for N'-alkylsubstituted amides of N-4-adamantyl-1-thiazolyl-2-oxamic acid has been developed and their synthesis has been performed. The possibility of formation of oxalic acid symmetric N,N'-dialkylamides has been theoretically grounded and confirmed experimentally while amidation of ethyl ester of N-4-(adamantly-1)-thiazolyl-2-oxaminic acid by alkylamines. The synthesis of N-4-(adamantly-1)-thiazolyl-2- and adamantly-1-amids of 1-R-2-oxo-4-hydroxyquinoline-3-carboxylic acids has been carried out. The effective purification method of such compounds from heavy metals salts has been offered. The ability of adamantly-1-amides of 1-R-2-oxo-4-hydroxyquinoline-3-carboxylic acids to form solvates with propanol-2 has been shown. The antituberculosis activity of all synthesized adamantan-containing amidated derivatives of oxalic and 1-R-2-oxo-4-hydroxyquinoline-3-carboxylic acid has been studied. As the result of the microbiological studies performed N'-nonylamide of N-4-(adamantly-1)-thiazolyl-2. oxaminic acid has been recommended for deeper research as a potential antituberculosis medication

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