50709-33-6Relevant articles and documents
Design, Synthesis, and Antifungal Activity of 2,6-Dimethyl-4-aminopyrimidine Hydrazones as PDHc-E1 Inhibitors with a Novel Binding Mode
Zhou, Yuan,Zhang, Shasha,Cai, Meng,Wang, Kaixing,Feng, Jiangtao,Xie, Dan,Feng, Lingling,Peng, Hao,He, Hongwu
, p. 5804 - 5817 (2021/06/25)
A series of novel 2,6-dimethyl-4-aminopyrimidine hydrazones 5 were rationally designed and synthesized as pyruvate dehydrogenase complex E1 (PDHc-E1) inhibitors. Compounds 5 strongly inhibited Escherichia coli (E. coli) PDHc-E1 (IC50 values 0.94-15.80 μM). As revealed by molecular docking, site-directed mutagenesis, enzymatic, and inhibition kinetic analyses, compounds 5 competitively inhibited PDHc-E1 and bound in a "straight"pattern at the E. coli PDHc-E1 active site, which is a new binding mode. In in vitro antifungal assays, most compounds 5 at 50 μg/mL showed more than 80% inhibition against the mycelial growth of six tested phytopathogenic fungi, including Botrytis cinerea, Monilia fructigena, Colletotrichum gloeosporioides, andBotryosphaeria dothidea. Notably, 5f and 5i were 1.8-380 fold more potent against M. fructigena than the commercial fungicides captan and chlorothalonil. In vivo, 5f and 5i controlled the growth of M. fructigena comparably to the commercial fungicide tebuconazole. Thus, 5f and 5i have potential commercial value for the control of peach brown rot caused by M. fructigena.
Ticyclic compd. and pharmaceutical composition containing the same
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Paragraph 0053; 0058, (2016/10/08)
PROBLEM TO BE SOLVED: To provide a compound which provides EP3 receptor antagonism, and a pharmaceutical composition which contains the compound and is for prevention against and treatment of prostaglandin mediated disorders. SOLUTION: There is disclosed the compound represented by general formula (I), where R1and R2are a hydrogen atom, a lower alkyl group, a lower haloalkyl group, a lower alkoxy group, or a halogen atom, R3is a monocyclic or bicyclic aromatic ring or heterocyclic ring, or a cyclo ring, R4is a monocyclic or bicyclic aromatic ring or heterocyclic ring, X is -CH2- or a carbon atom having a lower alkyl group, Y is -CH2CH2-(CH2)m- or -CR5=CR6-(CH2)m- (R5and R6may be identical or different and a hydrogen atom or a halogen atom), -O-CH2-(CH2)m-, (cyclo ring (1-5 carbons))-(CH2)m-, or (monocyclic or bicyclic aromatic ring)-(CH2)m-, where m is 0-5, Z is a bond or -SO2-, and n is 0-5. COPYRIGHT: (C)2013,JPO&INPIT
Design, synthesis, crystal structures, and insecticidal activities of eight-membered azabridge neonicotinoid analogues
Xu, Renbo,Xia, Rui,Luo, Ming,Xu, Xiaoyong,Cheng, Jiagao,Shao, Xusheng,Li, Zhong
, p. 381 - 390 (2014/02/14)
Three series of novel azabridge neonicotinoid analogues were designed and synthesized, which were constructed by starting material A, glutaraldehyde, and primary amine hydrochlorides (aliphatic amines, phenylhydrazines, and anilines). Most of the eight-membered azabridge compounds presented higher insecticidal activities than oxabridged compound B against cowpea aphid (Aphis craccivora) and brown planthopper (Nilaparvata lugens). Compared with imidacloprid, some azabridged compounds exhibited excellent insecticidal activity against brown planthopper. The crystal structures and bioassay indicated that changing bridge atoms from O to N could lead to entirely different conformations, which might be the important influential factor of the bioactivities.