40447-13-0Relevant articles and documents
Novel carboxylated pyrroline-2-one derivatives bearing a phenylhydrazine moiety: Design, synthesis, antifungal evaluation and 3D-QSAR analysis
Chen, Min,Zhang, Lizhi,Lu, Aimin,Wang, Xiaobin,Si, Weijie,Yan, Jinghua,Yang, Chunlong
, (2020/09/09)
Aiming to discover novel high-efficient antifungal leads that possess an innovative action mechanism, twenty-three carboxylated pyrroline-2-one derivatives, bearing a phenylhydrazine moiety, were rationally designed and firstly prepared in this letter. The in vitro bioassays showed that most of the compounds possessed excellent antifungal effects with the EC50 values of less than 1 μg/mL against the phytopathogenic fungi Fusarium graminearum (Fg), Botrytis cinerea (Bc), Rhizoctonia solani (Rs) and Colletotrichum capsici (Cc). The further bioassays showed that the compound 6u showed the comparable in vivo control effect with carbendazim against fusarium head blight and rice sheath blight. The 3D-QSAR model revealed the pivotal effects of a bulky electron-donating group at the 1-position of pyrrole ring, a bulky electron-withdrawing group at the 4-position of phenyl ring and a small alkyl at the carbonate group on the anti-Rs activities of target compounds. The abnormal mycelial morphology and delayed spore germination were observed in the treatments of compound 6u. Given the excellent and broad-spectrum antifungal effects the target compounds have, we unfeignedly anticipated that the above finding could motivate the discovery of high-efficient antifungal leads, which might possess an innovative action mechanism against phytopathogenic fungi.
Soluble Polymer-Supported Synthesis of α-Amino Acid Derivatives
Hu, Chunling,Chen, Zuxing,Yang, Guichun
, p. 219 - 224 (2007/10/03)
A practical and efficient synthesis of N-substituted α-amino acid derivatives on soluble polymer support is described.
(2-Oxo-1,2,3,5-tetrahydroimidazo-[2,1-B]quinazolinyl) oxyalkylamides properties having phosphodiosterase inhibiting
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, (2008/06/13)
Compounds according to the formula STR1 , its optical isomers, or a pharmaceutically acceptable salt thereof wherein: m and n are integers of 1 to 6; R1 is hydrogen or alkyl of 1 to 4 carbons; R2 is hydrogen or R1 and R2 are combined to form an oxo group; R3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or α-amino acid side chains; R4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl; R5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR6, halo, --NH2, --N(R6)2, --NHCOR6, --COOH, or --COO(R6) group wherein R6 is lower alkyl; phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with 1 or more lower alkyl, halo or lower alkoxy groups or an --NH2, --N(R6)2, --NHCOR6, --COOH, or --COOR6 group wherein R6 is lower alkyl; Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy; and Z is --OR7 or --NR7 R8 wherein R7 and R8 are independently hydrogen or lower alkyl.
