Vicentini, Chiara Beatrice published the artcilePyrazolo[3,4-c]isothiazole and isothiazolo[4,3-d]isoxazole derivatives as antifungal agents, Application In Synthesis of 1869-22-3, the publication is Pharmaceutical Biology (London, United Kingdom) (2011), 49(5), 545-552, database is CAplus and MEDLINE.
Fungal diseases due to zoopathogenic fungi and phytopathogenic fungi are increasing and among the substances used to combat fungi, azoles are of primary interest, both in agricultural fields and health and to void fungal resistance phenomena, the synthesis and tests of new derivatives are necessary. This article discusses the preparation and antifungal activity of pyrazolo[3,4-c]isothiazole and isothiazolo[4,3-d]isoxazole derivatives against three pathogenic fungi for plants and two opportunistic fungi in humans and plants. The synthesis of the target compounds [i.e., 6-[2-chloro-5-(trifluoromethyl)phenyl]-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine, 6-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine] was achieved using 2-cyano-3-ethoxy-2-butenethioamide as a starting material. The title compounds were evaluated against Magnaporthe grisea (phytopathogenic fungi), Pythium ultimum, Sclerotinia minor, Fusarium moniliforme (opportunistic strain ATCC 36541) and Trichoderma viride (opportunistic strain) and it was discovered that the fungi were sensitive toward the different azole-derivatives In general Magnaporthe grisea (T.T. Hebert Yaegashi & Udagawa) was the most sensitive fungus, being blocked almost entirely by a 4-chlorophenyl derivative [6-(4-chlorophenyl)-4-methyl-6H-pyrazolo[3,4-c]isothiazol-3-amine] even at 20 μμg/mL, a concentration at which the reference com. compound Tricyclazole was nearly ineffective. These findings demonstrate that the pyrazolo[3,4-c]isothiazole derivatives have a wide spectrum of activity on phytopathogenic and opportunistic fungi. In particular the 4-chloro derivative seems to have a great potential as new product to combat M. grisea in the agricultural field.
Pharmaceutical Biology (London, United Kingdom) published new progress about 1869-22-3. 1869-22-3 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Hydrazine,Amine,Benzene, name is 1-(2-Chloro-5-(trifluoromethyl)phenyl)hydrazine, and the molecular formula is C10H11NO4, Application In Synthesis of 1869-22-3.
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