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作者:Yadav Mange R , Shinde Anil K , Chouhan Bishram S ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry(IF 1.495), 2008, Vol.23 (2), pp.190-7PubMed
摘要:Cathepsins have been found to have important physiological roles. The implication of cathepsin L in various types of cancers is well established. In a search for selective cathepsin L inhibitors as anticancer agents, a series of 2-cyanoprrolidine peptidomimetics, carrying a nitri...
作者:Xia Li , Yuwen Liu , Jie Li ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry(IF 1.495), 2004, Vol.19 (4), pp.333-8PubMed
摘要:Na+/K+-ATPase (EC 3.6.1.3) is an important membrane-bound enzyme. In this paper, kinetic studies on Na+/K+-ATPase were carried out under mimetic physiological conditions. By using microcalorimeter, a thermokinetic method was employed for the first time. Compared with other method...
作者:Chen Qing-Xi , Song Kang-Kang , Wang Qin ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry(IF 1.495), 2003, Vol.18 (6), pp.491-6PubMed
摘要:The inhibition kinetics on the diphenolase activity of mushroom tyrosinase by some alkylbenzaldehydes has been investigated. The results show that the alkylbenzaldehydes assayed can lead to reversible inhibition to the enzyme; o-tolualdehyde and m-tolualdehyde are mixed-type inhi...
作者:Monti Simona Maria , Meccariello Angela , Ceruso Mariangela ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.255-259PubMed
摘要:The two β-carbonic anhydrases (CAs, EC 4.2.1.1) from the pathogenic bacterium Brucella suis, BsuCA1 and BsuCA2, were investigated for their inhibition profile with a series of pyridine-3-sulphonamide derivatives incorporating 4-hetaryl moieties. BsuCA1 was effectively inhibi...
作者:Chen Yao , Zhu Jie , Mo Jun ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.290-302PubMed
摘要:Small molecule cholinesterases inhibitor (ChEI) provides an effective therapeutic strategy to treat Alzheimer's disease (AD). Currently, the discovery of new ChEI with multi-target effect is still of great importance. Herein, we report the synthesis, structure-activity relat...
作者:Xie Xianrui , Cong Wei , Zhao Feng ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.98-105PubMed
摘要:Twenty-four novel 5-phenyl-1,3,4-oxadiazole-2-thiol (POT) analogues, benzo[d]oxazole-2-thiol, benzo[d]thiazole-2-thiol and 5-methyl-1,3,4-thiadiazole-2-thiol-substituted N,N-bis(2-hydroxyethyl) quaternary ammonium salts (QAS) (5a-d, 6a-d, 7a-d, 10a-d, 13a-d, 16a-d) were prep...
作者:Gao Xiao-Hui , Liu Lin-Bo , Liu Hao-Ran ...
来源:[J].Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.110-114PubMed
摘要:A series of benzamide and picolinamide derivatives containing dimethylamine side chain (4a-4c and 7a-7i) were synthesised and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity in vitro. Structure-activity relationship investigatio...
作者:Kato Eisuke , Kawakami Kazuhiro , Kawabata Jun
来源:[J].Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.106-109PubMed
摘要:Dipeptidyl peptidase 4 (DPP-4) inhibitors are used for the treatment of type-2 diabetes mellitus. Various synthetic inhibitors have been developed to date, and plants containing natural DPP-4 inhibitors have also been identified. Here, 13 plant samples were tested for their DPP-4...

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