Vlasenko Y. Synthesis, chemical properties and biological activity of 3,5-dіаmіnо-thiophenes with electron-withdrawing substitutes in positions 2 and 4

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0408U003044

Applicant for

Specialization

  • 15.00.02 - Фармацевтична хімія та фармакогнозія

30-05-2008

Specialized Academic Board

Д64.605.01

Essay

For the first time a „one-pot" technology of synthesis of substituted 3,5-diaminothiophenes has been developed through interaction substituted acetonitriles, arylisothiocyanates and substituted phenacylhalogenides. For the first time salts of N,S-acetalketenes and DBU have been obtained and studied. A possibility of bringing of different substitutes in positions 2 and 4 have been studied. Properties of 3,5-diaminothiophenes in reaction of acylation have been studied. For the first time 2-nitro-3,5-diaminothiophenes from inters 3,5-diamino-thiophenes and nitrosating reagents have been synthesized and the probable mechanism of carrying reaction have been proposed. 280 unentered compounds have been synthesized. For the first time a virtual screening of combinatorial library of substituted 3,5-diamino-thiophenes has been carried out using program PASS. A pharmacologic screening has been carried out and analgesic, antimicrobial, hypolipidemic and anti-inflammatory activities of 3,5-diamino-thiophene derivatives have been studied.

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