Synthesis and biological activity of new heterocyclic structures: [1,3]thiazino[2,3-i]purine, thiazolo[3,2-c] [1,2,3]triazolo[4,5-e]pyrimidine and [1,2,3]triazolo [4', 5': 4,5] pyrimido[6,1-b][1,3]thiazine

Farmaco. 1992 Oct;47(10):1315-22.

Abstract

Some derivatives of thiazolo[3,2-c]pyrimidine, pyrimido[6,1-b][1,3]thiazine, thiazolo[2,3-i]purine, [1,3]thiazino[2,3-i]purine, thiazolo[3,2-c][1,2,3]triazolo[4,5-e]pyrimidine and [1,2,3]triazolo[4',5':4,5]pyrimido[6,1-b][1,3]thiazine were prepared. The compounds were tested for antimicrobial and antimycotic activity on a number of strains, namely, Escherichia coli, Proteus vulgaris, P. mirabilis, Pseudomonas aeruginosa, Salmonella sp., Staphylococcus aureus, Streptococcus faecalis, Bacillus subtilis, Sarcina lutea, Candida albicans, Aspergillus sp., and for antiviral activity on Herpes simplex virus, Type 1 (HSV-1), Vesicular stomatitis virus (VSV) and Coxsackievirus B5 (CoxB5). The compounds proved to be devoid of activity against viruses, mycetes and gram-negative bacteria, while some of them exhibited a modest activity against gram-positive bacterial strains.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / pharmacology
  • Bacteria / drug effects
  • Fungi / drug effects
  • Isomerism
  • Microbial Sensitivity Tests
  • Purines / chemical synthesis*
  • Purines / pharmacology
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Thiazines / chemical synthesis*
  • Thiazines / pharmacology
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology
  • Vero Cells
  • Viral Plaque Assay
  • Viruses / drug effects

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Antifungal Agents
  • Antiviral Agents
  • Purines
  • Pyrimidines
  • Thiazines
  • Thiazoles
  • Triazoles
  • 2,3,8,9-tetrahydro-2-thioxo-7H-(1,3)thiazino(2,3-i)purin-5-(1H)-one
  • 7H-8,9-dihydro-(1,2,3)triazolo(4',5'-4,5)pyrimido(6,1-b)(1,3)thiazine-5(1H)-one
  • thiazolo(3,2-c)(1,2,3)triazolo(4,5-e)pyrimidine