title: Biological activity of tropolone.
abstract: 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 (IC(50)) being 2.73 x 10(-6) M. This inhibitory activity was as high as that of 2 (IC(50): 2.76 x 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 microg/ml. In particular, 1 showed strong antifungal activity on Pythium aphanidermatum IFO-32440 (MIC: 6.0 microg/ml).
authors.affiliation: Osaka Organic Chemical Industry, Ltd, Osaka, Japan.
authors.forename: Yasuhiro
authors.initials: Y
authors.lastname: Morita
authors.forename: Eiko
authors.initials: E
authors.lastname: Matsumura
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Okabe
authors.forename: Mitsunobu
authors.initials: M
authors.lastname: Shibata
authors.forename: Masaaki
authors.initials: M
authors.lastname: Sugiura
authors.forename: Tatsuhiko
authors.initials: T
authors.lastname: Ohe
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tsujibo
authors.forename: Nakao
authors.initials: N
authors.lastname: Ishida
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Inamori
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D007313:Insecta / Q000187:drug effects / Q000502:physiology; D007306:Insecticides / Q000737:chemistry / Q000494:pharmacology*; D011775:Pythium / Q000187:drug effects / Q000502:physiology; D014334:Tropolone / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D007306:Insecticides; D014334:Tropolone