The synthesis and physicochemical properties of new derivatives of 5-r-phenylamino-2-mercapto-1,3,4-thiadiazole

Authors

  • I. V. Sych National University of Pharmacy, Ukraine
  • L. O. Perekhoda National University of Pharmacy, Ukraine
  • Z. G. Ieromina National University of Pharmacy, Ukraine
  • L. O. Grinevich National University of Pharmacy, Ukraine
  • N. P. Kobzar National University of Pharmacy, Ukraine
  • I. V. Drapak Lviv National Medical University named after Danylo Halytsky, Ukraine

DOI:

https://doi.org/10.24959/nphj.16.2074

Keywords:

synthesis, 1, 3, 4-thiadiazole, 1H NMR-spectroscopy

Abstract

With the aim of obtaining new biologically active substances the synthesis of amides of 5-R-phenylamino-1,3,4-thiadiazole-2-yl-thioacetate acid and 5-phenylamino-1,3,4-thiadiazole-2-yl-thio-1-phenon has been conducted. As initial substances 5-R-phenylamino-2-mercapto-1,3,4-thiadiazoles, the corresponding analides of chloracetate acid and chloracetate phenon were used. The reaction of alkylation was conducted in the ethanol medium in the presence of potassium hydroxide. The structure of the compounds synthesized has been confirmed by the method of 1H NMR-spectroscopy. The physicochemical properties and the pharmacological potential of the substances synthesized are discussed. According to the results of calculation methods of prediction of the biological activity (PASSOnline) the probable types of the biological activity of the substances synthesized have been estimated. In compliance with the data of the PASSOnline computer-based prognosis the antineoplastic action (STAT inhibitor of transcription factors) is principally inherent for most compounds of this class.

Author Biographies

I. V. Sych, National University of Pharmacy

graduate student of the Department of Medicinal Chemistry

L. O. Perekhoda, National University of Pharmacy

professor of the Department of Medicinal Chemistry

Z. G. Ieromina, National University of Pharmacy

assistent professor of the Department of Medicinal Chemistry

L. O. Grinevich, National University of Pharmacy

assistent of the Department of Medicinal Chemistry

N. P. Kobzar, National University of Pharmacy

assistent professor of the Department of Medicinal Chemistry

I. V. Drapak, Lviv National Medical University named after Danylo Halytsky

assistent professor of the Department of general, bioinorganic, physical and colloidal chemistry

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Published

2016-03-11

Issue

Section

Synthesis and Analysis of Biologically Active Substances