91419-48-6Relevant articles and documents
Design, Synthesis, and Fungicidal Activities of Novel Piperidyl Thiazole Derivatives Containing Oxime Ether or Oxime Ester Moieties
Bian, Qiang,Zhao, Rui-Qi,Peng, Xing-Jie,Gao, Li-Jie,Zhou, Guo-Na,Yu, Shu-Jing,Zhao, Wei-Guang
, p. 3848 - 3858 (2021/05/04)
To explore the influence of the positions of the two nitrogen atoms on the thiazole ring and the isoxazoline ring on the activity, a series of novel piperidyl thiazole derivatives containing oxime ether and oxime ester moieties with two nitrogen atoms on the same or opposite sides have been designed, synthesized, and first evaluated for their fungicidal activities against Phytophthora capsici in vitro. The bioassay results showed that the target compounds possessed moderate to good fungicidal activities against P. capsici, among which oxime ether compound 11b shows the highest fungicidal activity in vitro (EC50 = 0.0104 μg/mL) which is higher than dimethomorph (EC50 = 0.1148 μg/mL) and diacetylenyl amide (EC50 = 0.040 μg/mL). Compared with oxime ether compounds (the two nitrogen atoms are on the opposite sides), the activities of oxime ester compounds were significantly reduced. It is different from the commercial fungicide fluoxapiprolin, and the activities of the compounds with the two nitrogen atoms on the same side were significantly reduced compared to the compounds with the two nitrogen atoms on the opposite sides. Moreover, compounds 11b, 11d, 11e, and 11g showed moderate to good antifungal activities in vivo against Phytophthora capsici, Pseudoperonospora cubensis, and Phytophthora infestans. Scanning electron microscopy of compound 11b on the hyphae morphology showed that compound 11b might cause mycelial abnormalities of P. capsici.
Piperidyl tetrahydrobenzothiazole oxime ether derivative and application thereof
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Paragraph 0033; 0062-0063, (2020/09/23)
The invention relates to a piperidyl tetrahydrobenzothiazole oxime ether derivative as shown in a general formula (I) and application of the piperidyl tetrahydrobenzothiazole oxime ether derivative asa bactericide. The compound represents a novel bactericide structure type, has excellent sterilization activity and can be used for preventing and treating diseases such as downy mildew, late blightand downy mildew generated by oomycetes pathogenic bacteria, particularly cucumber downy mildew, grape downy mildew, cabbage downy mildew, tomato late blight, potato late blight, pepper late blight, litchi downy blight and soybean phytophthora root rot. The compound is also suitable for sclerotinia sclerotiorum, ring rot, gray mold, banded sclerotial blight and the like. The compound disclosed bythe invention can be directly used, can also be used together with an agriculturally acceptable carrier, and can also be compounded with other bactericides for use.
Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists
Kim, Hyojin,Cho, Suk Joon,Yoo, Minjin,Kang, Seung Kyu,Kim, Kwang Rok,Lee, Hwan Hee,Song, Jin Sook,Rhee, Sang Dal,Jung, Won Hoon,Ahn, Jin Hee,Jung, Jae-Kyung,Jung, Kwan-Young
supporting information, p. 5213 - 5220 (2017/11/21)
A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.
