96748-34-4Relevant academic research and scientific papers
Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold
Flaherty, Daniel P.,Simpson, Denise S.,Miller, Melissa,Maki, Brooks E.,Zou, Beiyan,Shi, Jie,Wu, Meng,McManus, Owen B.,Aubé, Jeffrey,Li, Min,Golden, Jennifer E.
, p. 3968 - 3973 (2014/09/03)
TASK-1 is a two-pore domain potassium channel that is important to modulating cell excitability, most notably in the context of neuronal pathways. In order to leverage TASK-1 for therapeutic benefit, its physiological role needs better characterization; however, designing selective inhibitors that avoid the closely related TASK-3 channel has been challenging. In this study, a series of bis-amide derived compounds were found to demonstrate improved TASK-1 selectivity over TASK-3 compared to reported inhibitors. Optimization of a marginally selective hit led to analog 35 which displays a TASK-1 IC 50 = 16 nM with 62-fold selectivity over TASK-3 in an orthogonal electrophysiology assay.
Optimization and antifungal activity of amide analogues
Feng, Hui,Leng, Li,Liu, Jia,Tang, Yuanmou,Tang, Pengcheng,Zhang, Chixiang,Tang, Xioarong,Jiao, Shirong
, p. 4029 - 4031 (2013/05/09)
Using salicylic acid as a lead compound, a series of its analogues (compounds 1-16) were designed and synthesized. Their activity of antipathogenic fungi of plants has been evaluated in the laboratory. The results showed that these compounds had certain antifungal activity against Sclerotinia sclerotiorum and Bipolaris maydis (Nisikado et Miyake) Shoem. Among them, the inhibition of growth for 2-(3- fluorophenylcarbamoyl)phenyl acetate (1) and 2-(3-chlorophenylcarbamoyl)phenyl acetate (2) reached 91.1 %, 92.8 % and 90.1 %, 90.1 % at a concentration of 100 mg L-1, respectively.
N-Acylthiourea and N-Acylurea Inhibitors of the Hedgehog Protein Signalling Pathway
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Page/Page column 14, (2011/11/13)
The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or a
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS
Zhou, Ya,Rodriguez, Alice L.,Williams, Richard,Weaver, C. David,Conn, P. Jeffrey,Lindsley, Craig W.
scheme or table, p. 6502 - 6506 (2010/05/17)
This Letter describes the discovery and SAR of three novel series of mGluR5 non-competitive antagonists/negative allosteric modulators (NAMs) not based on manipulation of an MPEP/MTEP chemotype identified by a functional HTS approach. This work demonstrates fundamentally new mGluR5 NAM chemotypes with submicromolar potencies, and further examples of a mode of pharmacology 'switch' to provide PAMs with a non-MPEP scaffold.
