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Biological Activity of Tropolone

2003; Pharmaceutical Society of Japan; Volume: 26; Issue: 10 Linguagem: Inglês

10.1248/bpb.26.1487

1347-5215

Yasuhiro Morita, Eiko Matsumura, Toshihiro Okabe, Mitsunobu Shibata, Masaaki Sugiura, Tatsuhiko Ohe, Hiroshi Tsujibo, Nakao Ishida, Yoshihiko Inamori,

Synthesis of Organic Compounds

Tropolone (1) showed strong insecticidal activity on Tyrophagus putrescentiae and Dermatophagoides farinae. The insecticidal effect of 1 on both insects was stronger than that of hinokitiol (2, 4-isopropyltropolone: major component of Thujopsis dolabrata SIEB. et ZUCC. hondai MAKINO). The insecticidal activity of both compounds was higher than that of N,N-diethyl-m-toluamide (DEET), used as a positive control. Compound 1 had potent insecticidal activity against Coptotermes formosanus, although its activity was much lower than that of commercial chloropyrifos. Like 2, 1 showed the inhibitory activity toward metalloproteases such as carboxypeptidase A, collagenase and thermolysin and their inhibitory activities were much higher than that of 1,10-phenanthroline, used as a positive control. The inhibitory activity of 1 on carboxypeptidase A was especially high, its 50% inhibitory concentrations (IC50) being 2.73×10−6 M. This inhibitory activity was as high as that of 2 (IC50: 2.76×10−6 M). Compound 1 inhibited the growth of seven kinds of plant-pathogenic fungi and their minimum inhibitory concentration (MIC) values were in the range of 6.0—50.0 μg/ml. In particular, 1 showed strong antifungal activity on Pythium aphanidermatum IFO-32440 (MIC: 6.0 μg/ml).