Synthesis and antimicrobial activity of 3-benzyl-5-methyl-4-oxo-2-thioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-сarboxylic acid amides

Authors

  • Сергій Віталійович Власов National University of Pharmacy Pushkinskaya str., 53, Kharkov, Ukraine, 61002, Ukraine
  • Валентин Петрович Черних National University of Pharmacy Pushkinskaya str., 53, Kharkov, Ukraine, 61002, Ukraine

DOI:

https://doi.org/10.15587/2519-4852.2016.72700

Keywords:

thiophene, pyrimidine, carboxylic acids, amides, imidazolides, mercaptans, alkylation, antimicrobial agents

Abstract

Aim. Targeted preparation of the novel antimicrobial agents among the derivatives of 2-thiothieno[2,3-d]pyrimidine-6-carboxylic acids.

Materials and methods of research. The routine methods of organic synthesis and structural chemistry, the screening methods recommended by WHO for antimicrobial activity studies were used for this work.

Results. The series of the novel amides of 3-benzyl-5-methyl-4-oxo-2-thioxo-1,2,3,4-terahydrothieno[2,3-d]pyrimidine-6-carboxylic acid has been performed using the 1,1'-carbonyldiimidazole promoted interaction of the corresponding acid with amines in the DMF media and their antimicrobial activity was studied.

Conclusions. The study for the amides obtained allowed identification of some derivatives with the wide range of antibacterial activity and no influence on the growth of Candida fungi; the ethyl ester of 3-benzyl-5-methyl-4-oxo-2-thioxo-1,2,3,4-terahydrothieno[2,3-d]pyrimidine-6-carboxylic acid was found to be the most active compound against the strains of Bacillus subtilis and Candida albicans

Author Biographies

Сергій Віталійович Власов, National University of Pharmacy Pushkinskaya str., 53, Kharkov, Ukraine, 61002

Candidate of chemical sciences, associate professor

Department of Organic Chemistry

Валентин Петрович Черних, National University of Pharmacy Pushkinskaya str., 53, Kharkov, Ukraine, 61002

Doctor of Pharmacy, Doctor of Chemistry, professor, academician of the National Academy of Sciences of Ukraine, Rector

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Published

2016-07-01

How to Cite

Власов, С. В., & Черних, В. П. (2016). Synthesis and antimicrobial activity of 3-benzyl-5-methyl-4-oxo-2-thioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-сarboxylic acid amides. ScienceRise: Pharmaceutical Science, (1 (1), 4–9. https://doi.org/10.15587/2519-4852.2016.72700

Issue

No. 1 (1) (2016)

Section

Pharmaceutical Science

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Copyright (c) 2016 Сергій Віталійович Власов, Валентин Петрович Черних

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