International Journal of Antimicrobial Agents
Volume 14, Issue 3 , Pages 203-207, April 2000

Synthesis and biological activity of N-acylphenothiazines

  • Noboru Motohashi

      Affiliations

    • Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose-shi, Tokyo 204-8588, Japan
    • Corresponding Author InformationCorresponding author. Tel.: +81-424-958953; fax: +81-424-958953
    • ,
  • Masami Kawase

      Affiliations

    • Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    • ,
  • Setsuo Saito

      Affiliations

    • Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan
    • ,
  • Teruo Kurihara

      Affiliations

    • Faculty of Science, Josai University, Saitama, Japan
    • ,
  • Kazue Satoh

      Affiliations

    • Analysis Center, School of Pharmaceutical Sciences, Showa University, Tokyo, Japan
    • ,
  • Hideki Nakashima

      Affiliations

    • Department of Microbiology and Immunology, Kagoshima University Dental School, Kagoshima, Japan
    • ,
  • Mariappan Premanathan

      Affiliations

    • Department of Microbiology and Immunology, Kagoshima University Dental School, Kagoshima, Japan
    • ,
  • Rieko Arakaki

      Affiliations

    • Department of Microbiology and Immunology, Kagoshima University Dental School, Kagoshima, Japan
    • ,
  • Hiroshi Sakagami

      Affiliations

    • Department of Dental Pharmacology, Meikai University School of Dentistry, Saitama, Japan
    • ,
  • Joseph Molnár

      Affiliations

    • Institute of Microbiology, Albert Szent-Györgyi Medical University, Dóm tér 10, H-6720 Szeged, Hungary

Abstract 

Previous studies have demonstrated the relationship between radical intensity and cytotoxic activity in water-soluble compounds. This relationship was investigated in lipophilic compounds. Several N-acylphenothiazines showed higher cytotoxic activity against human leukemic and squamous carcinoma cell lines than phenothiazine, the parent compound. Electron spin resonance (ESR) spectroscopy showed that these active compounds produced much lower amounts of radicals than phenothiazine. Several compounds failed to inhibit the cytopathic effects of human immunodeficiency virus (HIV) infection in MT-4 cells. It suggested that the radical-mediated-mechanisms has not involved in the induction of cytotoxic activity by lipophilic compounds, such as N-acylphenothiazines.

Keywords:  N-Acylphenothiazines, HL-60 cells, HSC-2 cells, Anti-HIV activity, Free radicals, Water-solubility

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PII: S0924-8579(99)00156-9

International Journal of Antimicrobial Agents
Volume 14, Issue 3 , Pages 203-207, April 2000

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