20689-54-7Relevant articles and documents
Diastereoselective intermolecular cobalt-catalyzed reductive aldol reactions of α,β-unsaturated amides with ketones
Lumby, Ralph J. R.,Joensuu, Pekka M.,Lam, Hon Wai
, p. 4367 - 4370 (2007)
Under cobalt catalysis, diethylzinc mediates the conjugate reduction of αβ-unsaturated amides to produce ethylzinc enolates that react with ketones in situ to produce tertiary alcohol-containing aldol products with up to >19:1 diastereoselectivity.
Design and synthesis novel amide derivatives containing an 1,3,4-oxadiazole moiety as potential antibacterial agents
Chen, Jixiang,Chen, Yifang,Luo, Xin,Wang, Yu,Xing, Zhifu
supporting information, (2022/02/17)
To find new antibacterial agents, 25 novel amide derivatives containing an 1,3,4-oxadiazole moiety were designed and synthesized, and their antibacterial activity against Xanthomonas oryzae pv. oryzicola (Xoc) and Xanthomonas oryzae pv. oryzae (Xoo) were tested. Interestingly, all target compounds showed excellent antibacterial activities against Xoc and Xoo. The EC50 values of compounds 1–25 against Xoc and Xoo were 1.2–4.0?mg/L and 0.5–2.3?mg/L, respectively, which were significantly superior to those of the thiodiazole copper (95.1 and 89.0?mg/L) and bismerthhibol (73.8 and 68.8?mg/L). For example, the EC50 values of compound 16 against Xoc and Xoo were 1.7 and 0.5?mg/L, respectively. Meanwhile, the curative and protection activity of compound 16 against rice bacterial leaf blight were 42.4% and 42.1%, respectively, which were superior to the control of jiahuangxianjunzuo (34.1% and 32.6%) and thiodiazole copper (33.0% and 27.1%). In addition, compound 16 might suppress the cell growth of Xoo by inhibiting the production of extracellular polysaccharide, the formation of biofilm, changes the cell membrane permeability, and cell surface morphology.
Quinoline derivative containing furyl and preparation method and application thereof
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Paragraph 0098-0102, (2021/05/08)
The invention belongs to the field of anti-cancer drugs, and particularly relates to a furyl-containing quinoline derivative and a preparation method and application thereof. The invention provides a compound as shown in the formula I, and a stereoisomer or pharmaceutically acceptable salt thereof. Compared with an existing antitumor drug, the compound disclosed by the invention has excellent antitumor activity on A431, SKOV3, SK-BR-3, BT474 and the like, and has a very good application prospect. In addition, the preparation method of the compound is low in cost, simple in step, mild in reaction condition, high in yield and easy for post-treatment.
Discovery and development of novel pyrimidine and pyrazolo/thieno-fused pyrimidine derivatives as potent and orally active inducible nitric oxide synthase dimerization inhibitor with efficacy for arthritis
Chen, Liu Zeng,Shu, Hai Yang,Wu, Jing,Yu, Yun Long,Ma, Duo,Huang, Xin,Liu, Ming Ming,Liu, Xin Hua,Shi, Jing Bo
, (2021/02/03)
In order to discover and develop drug-like anti-inflammatory agents against arthritis, based on “Hit” we found earlier and to overcome drawbacks of toxicity, twelve series of total 89 novel pyrimidine, pyrazolo[4,3-d]pyrimidine and thieno[3,2-d]pyrimidine derivatives were designed, synthesized and screened for their anti-inflammatory activity against NO and toxicity for normal liver cells (LO2). Relationships of balance toxicity and activity have been summarized through multi-steps, and title compounds 22o, 22l were found to show lower toxicity (against LO2: IC50 = 2934, 2301 μM, respectively) and potent effect against NO release (IR = 98.3, 97.67%, at 10 μM, respectively). Furthermore, compound 22o showed potent iNOS inhibitory activity with value of IC50 is 0.96 μM and could interfere stability and formation of the active dimeric iNOS. It's anti-inflammatory activity in vivo was assessed by AIA rat model. Furthermore, the results of metabolic stability, CYP, PK study in vivo, acute toxicity study and subacute toxicity assessment indicated this compound had good drug-like properties for treatment.
