500302-20-5Relevant articles and documents
FUSED CYCLIC UREA DERIVATIVES AS CRHR2 ANTAGONIST
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Paragraph 0150; 0290, (2019/11/04)
The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR1 and/or CRHR2 is involved.
Design, synthesis and antifungal activity of novel fenfuram-diarylamine hybrids
Wang, Hongyu,Gao, Xuheng,Zhang, Xiaoxiao,Jin, Hong,Tao, Ke,Hou, Taiping
supporting information, p. 90 - 93 (2016/12/09)
Ten novel fenfuram-diarylamine hybrids were designed and synthesized. And their antifungal activities against four phytopathogenic fungi have been evaluated in vitro and most of the compounds demonstrated a significant antifungal activities against Rhizoctonia solani and Sclerotinia sclerotiorum. Compound 5e exhibited the most potent antifungal activity against R. solani with an EC50value of 0.037 mg/L, far superior to the commercially available fungicide boscalid (EC50= 1.71 mg/L) and lead fungicide fenfuram (EC50= 6.18 mg/L). Furthermore, scanning electron microscopy images showed that the mycelia on treated media grew abnormally with tenuous, wizened and overlapping colonies compared to the negative control. Molecular docking studies revealed that compound 5e featured a higher affinity for succinate dehydrogenase (SDH) than fenfuram. Furthermore, it was shown that the 3-chlorophenyl group in compound 5e formed a CH-π interaction with B/Trp-206 and a Cl-π interaction with D/Tyr-128, rendering compound 5e more active than fenfuram against SDH.
Synthesis and biological evaluation of novel pyrazole carboxamide with diarylamine-modi?ed scaffold as potent antifungal agents
Zhang, Xiao-Xiao,Jin, Hong,Deng, Yuan-Jie,Gao, Xu-Heng,Li, Yong,Zhao, Yong-Tian,Tao, Ke,Hou, Tai-Ping
, p. 1731 - 1736 (2017/07/27)
Twenty-seven novel pyrazole carboxamides with diarylamine-modi?ed scaffold were designed, synthesized and characterized in detail via 1H NMR, 13C NMR, IR and ESI-HRMS. Preliminary bioassays showed that some of the target compounds exhibited good antifungal activity against Rhizoctonia solani, Rhizoctonia cerealis and Sclerotinia sclerotiorum. Among them, compound 9c-7 exhibited the highest antifungal activities against R. solani, R. cerealis and S. sclerotiorum in vitro with IC50 values of 0.013, 1.608 and 1.874?μg/mL, respectively. Notably, compound 9c-7 still presented the highest fungicidal activities against R. solani in vivo with an IC50 value of 22.21?μg/mL. Molecular docking simulation results reveal that compound 9c-7 binds well to the hydrophobic pockets of the receptor protein succinate dehydrogenase. This study suggests that compound 9c-7 could act as a potential fungicide to be used for further optimization.
A heterocyclic ligands containing compounds and methods for their preparation, application (by machine translation)
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Paragraph 0153-0157; 0158; 0159; 0160; 0162, (2016/10/08)
The present invention provides a compound containing heterocyclic ligands and its preparation method, an electroluminescent device. The present invention provides heterocycle-containing ligand compound, through the particular selection of heterocyclic ligands and different metal binding, can adjust the wavelength of the compound, the organic metal compound used in the organic electroluminescent device, to make the device light-emitting efficiency is improved, and the service life is long. (by machine translation)
Compound with heterocyclic ligand and preparation method and application thereof
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Paragraph 0106; 0107; 0108; 0109; 0110; 0111; 0112, (2016/10/08)
The invention provides a compound with a heterocyclic ligand and a preparation method and application thereof. According to the compound with the heterocyclic ligand, the specific heterocyclic ligand is selected to be combined with metal aluminum, so that after the obtained organic compound is applied to an organic light-emitting device, the light-emitting efficiency of the device is improved, and the service life is long.
Lithium compound with heterocyclic ligand and preparation method and application thereof
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Paragraph 0123; 0124; 0125; 0126; 0127, (2016/10/08)
The invention provides a lithium compound with a heterocyclic ligand and a preparation method and application thereof. According to the lithium compound with the heterocyclic ligand, the specific heterocyclic ligand is selected to be combined with metal lithium, so that after the obtained organic lithium compound is applied to an organic light-emitting device, the light-emitting efficiency of the device is improved, and the service life is long.
Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-Aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3 H)-yl]-1-(methylamino)butan-2- ols (WYE-103231)
O'Neill, David J.,Adedoyin, Adedayo,Alfinito, Peter D.,Bray, Jenifer A.,Cosmi, Scott,Deecher, Darlene C.,Fensome, Andrew,Harrison, Jim,Leventhal, Liza,Mann, Charles,McComas, Casey C.,Sullivan, Nicole R.,Spangler, Taylor B.,Uveges, Albert J.,Trybulski, Eugene J.,Whiteside, Garth T.,Zhang, Puwen
experimental part, p. 4511 - 4521 (2010/08/20)
Structural modification of a virtual screening hit led to the identification of a new series of 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol- 1(3H)-yl]-1-(methylamino)butan-2-ols which are potent and selective inhibitors of the norepinephrine transporter over both the serotonin and dopamine transporters. One representative compound S-17b (WYE-103231) had low nanomolar hNET potency (IC50 = 1.2 nM) and excellent selectivity for hNET over hSERT (>1600-fold) and hDAT (>600-fold). S-17b additionally had a good pharmacokinetic profile and demonstrated oral efficacy in rat models of ovariectomized-induced thermoregulatory dysfunction and morphine dependent flush as well as the hot plate and spinal nerve ligation (SNL) models of acute and neuropathic pain.