207849-74-9Relevant articles and documents
Pine Rosin as a Valuable Natural Resource in the Synthesis of Fungicide Candidates for Controlling Fusarium oxysporum on Cucumber
Mao, Shiying,Wu, Chengyu,Gao, Yanqing,Hao, Jin,He, Xiaohua,Tao, Pan,Li, Jian,Shang, Shibin,Song, Zhanqian,Song, Jie
, p. 6475 - 6484 (2021/06/28)
To improve the effect of pine rosin in plant fungicides, four series of dehydroabietyl-1,3,4-thiadiazole derivatives from the natural product rosin were synthesized. Based on the evaluation of the in vitro antifungal activity against Sclerotinia sclerotiorum, Botrytis cinerea, Fusarium oxysporum, and Magnaporthe oryzae, rosin-based 1,3,4-thiadiazole compounds containing thiophene heterocycles were screened. Notably, compound 3e [dehydroabietyl-(1,3,4-thiadiazol-2-yl)-5-nitrothiophene-2-carboxamide] exhibited excellent antifungal property against F. oxysporum with an EC50 of 0.618 mg/L, which was lower than that of the positive control carbendazim (0.649 mg/L). The in vivo antifungal activity results showed that 3e exerted a protective effect on cucumber plants. Physiological and biochemical studies showed that the primary mechanism of action of compound 3e on F. oxysporum was it changed the mycelial morphology, increased the cell membrane permeability, and inhibited the synthesis of ergosterol in the mycelia. Furthermore, the quantitative structure-activity relationship studies revealed that the frontier orbital energy in the molecule had a key role in the antifungal activity through the conjugation and electrostatic interaction between compound 3e and the receptors of the target. Thus, the present study highlighted the application of rosin-based fungicidal candidates and exploited efficient plant pesticides for sustainable crop production.
INHIBITOR OF CASEIN KINASE 1DELTA AND CASEIN KINASE 1E
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, (2013/06/05)
There is provided a novel oxazolone derivative having inhibitory activity against casein kinase 1δ and casein kinase 1ε. In addition, the present inhibitor inhibits casein kinase 1δ and casein kinase 1ε, and thus there is also provided a pharmaceutical agent useful for the treatment and/or prevention of diseases, with the pathological conditions of which the activation mechanism of casein kinase 1δ or casein kinase 1ε is associated. There is further provided a pharmaceutical agent useful for the treatment of particularly, circadian rhythm disorder (including sleep disorder), central neurodegenerative disease, and cancer. An inhibitor of casein kinase 1δ and casein kinase 1ε comprising, as an act ingredient, an oxazolone derivative represented by the following general formula (1), a salt thereof, a solvate thereof, or a hydrate thereof: wherein X represents a halogen atom (which may be any one of a fluorine atom, a chlorine atom, a bromine atom, and an iodine atom).
Processes and intermediates for preparing 2-fluorothiophene derivatives
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, (2008/06/13)
A process for the preparation of the compound of the formula: wherein R1 is OH, which comprises the steps of a) treating the compound of the formula: with an inorganic fluoride, of the formula M2F wherein M2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R4P+Z- and a compound of the formula R5vic (COW)2 wherein R4 and R5 are each selected from optionally substituted (C6-C10) aryl and optionally substituted (C1-C6) alkyl, and W is halo; to form the compound of the formula: and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, and ii) treating the product of step i) with a mineral acid. A compound of the formula: wherein R1 is selected from the group consisting of, halo, R7O, R7COO and N(R8)2 wherein R7 is (C1-C6)alkyl or (C6-C10)aryl and each R8 is selected from hydrogen and R7 with the proviso that R7 is not methyl when R1 is R7O.
