Anti-infective and herbicidal activity of N-substituted 2-aminobenzothiazoles

Bioorg Med Chem. 2012 Dec 15;20(24):7059-68. doi: 10.1016/j.bmc.2012.10.007. Epub 2012 Oct 17.

Abstract

In this study, a series of N-substituted 2-aminobenzothiazoles was prepared according to a recently developed method. Twelve compounds were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the discussed compounds was also performed against fungal, bacterial and mycobacterial species. The biological activities of some compounds were comparable or higher than the standards phenoxymethylpenicillin or pyrazinamide. The most effective compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. For all compounds, the structure-activity relationships are discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis
  • Anti-Infective Agents / chemistry*
  • Anti-Infective Agents / pharmacology*
  • Antifungal Agents / metabolism
  • Antifungal Agents / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Benzothiazoles / chemical synthesis
  • Benzothiazoles / chemistry*
  • Benzothiazoles / pharmacology*
  • Cell Line, Tumor
  • Chloroplasts / drug effects
  • Drug Screening Assays, Antitumor
  • Herbicides / chemical synthesis
  • Herbicides / chemistry*
  • Herbicides / pharmacology*
  • Humans
  • Microbial Sensitivity Tests
  • Spinacia oleracea
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Benzothiazoles
  • Herbicides