Yanchenko V. The synthesis and properties of4-ammo-3-mercapto-4H-l ,2,4-triazole derivative

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0405U002235

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

22-04-2005

Specialized Academic Board

Д64.605.01

Essay

The thesis is dedicated to the development of methods of synthesis triazolbearing compounds originating from 4-amino-3-mercapto-4H-l,2,4-triazoIe. Conditions of obtaining Nl-aryl-2-(5-alkyl-4-amino-4H-1,2,4-triazol-3-ylthio) acetamides have been studied at the result of the current work and the possibility of their ring closer into 6-arylamino-7H-[l,2,4]triazoIo[3,4-b][l,3,4]-thiadiazines was shown. The structure of products of condensation 4-arylmethylidenamino-4H-l,2,4-triazol-3-ylthiols with bifunctional compounds was investigated. The opportunity of double bond transferring in azomethinic group of 6-aryl-7H-[l,2,4]triazolo[3,4-b][l,3,4]thiadiazine with formation of isomeric 5H-[l,2,4]triazolo[3,4-b][l,3,4]thiadiazines was proved. The possibility of the synthesis of substituted [1,2,4]triazolo[4,3-b]pyridazines by cyclocondensation of 4H-triazolyl-3-thiol derivatives with 2,4-pentanedione was established. Unexpected direction of 4-amino-5-trifluormethyl-4H-triazolyl-3-thiol reaction with dehydroacetic acid was shown. For all synthesized compounds anti-inflammatory, analgesic, fungicidal, antimicrobial, antioxidative and antiviral activity was investigated. Ethyl 2-(4-amino-5-trifluoromethyl-4H-1,2,4-triazol-3-ylsulfanylmethylcarboxamido)-5,6-dihydro-4H-cyclopenta[b]thiophene-3-carboxylate, which showed a anti-inflammatory activity, has been recommended for the ofurther pharmacological studying.

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