Dzharadat N. Synthesis of potential antituberculosis agent on the basis of 1r-2-oxo-4-hydroxyquinoline-3-carboxilic acids hydrazides

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0400U002535

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

06-10-2000

Specialized Academic Board

Д64.605.01

Essay

The reaction of 1-R-2-oxo-4-hydroxyquinoline-3-carboxylic acids hydrazides with ethyl orthoformate has been studied The isolated ethoxymethylidenhydrazides were found to be transformed into ethyl esters of the corresponding quinoline-3-carboxylic acids under the influence of ethyl ortoformate excess and into symmetric N,N'-di-(1-alkyl-2-oxo-4-hydroxyquinolinoyl-3)-hidrazines under thermolysis conditions. The most optimal conditions for obtaining N-alkylantranylic acids which are the key structures in the synthesis of 2-oxo-4-hydroxyquinolines have been proposed. The synthensis of benzylidenhydrazides and (2'-alkyl-4'-oxoquinazolone-3'-yl)amides of 1R-2-oxo-4-hydroxyquinoline-3-carboxylic acids has been carried out. Benzylidenhydrazide of 1-hexyl-2-oxo-4-hydroxyquinoline-3-carboxylic acid as a potential drug for treating tuberculosis and non-tuberculosis mycobacterioses was recommended for further pharmacological research.

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