27943-07-3Relevant articles and documents
Discovery, synthesis and characterization of a series of (1-alkyl-3-methyl-1H-pyrazol-5-yl)-2-(5-aryl-2H-tetrazol-2-yl)acetamides as novel GIRK1/2 potassium channel activators
Sharma, Swagat,Kozek, Krystian A.,Abney, Kristopher K.,Kumar, Sushil,Gautam, Nagsen,Alnouti, Yazen,David Weaver,Hopkins, Corey R.
, p. 791 - 796 (2019/02/06)
The present study describes the discovery and characterization of a series of 5-aryl-2H-tetrazol-3-ylacetamides as G protein-gated inwardly-rectifying potassium (GIRK) channels activators. Working from an initial hit discovered during a high-throughput screening campaign, we identified a tetrazole scaffold that shifts away from the previously reported urea-based scaffolds while remaining effective GIRK1/2 channel activators. In addition, we evaluated the compounds in Tier 1 DMPK assays and have identified a (3-methyl-1H-pyrazol-1-yl)tetrahydrothiophene-1,1-dioxide head group that imparts interesting and unexpected microsomal stability compared to previously-reported pyrazole head groups.
PYRIDINE DERIVATIVE AS ASK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0104-0105; 0110, (2019/12/05)
Disclosed in the present invention are a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and also disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
Efficient synthesis of tetrazole hemiaminal silyl ethers via three-component hemiaminal silylation
Xie, Ming-Sheng,Cheng, Xuan,Chen, Yang-Guang,Wu, Xiao-Xia,Qu, Gui-Rong,Guo, Hai-Ming
supporting information, p. 6890 - 6894 (2018/10/17)
An efficient route to construct 2,5-disubstituted tetrazole hemiaminal silyl ethers via one-pot three-component hemiaminal silylation of 5-substituted tetrazoles, aldehydes, and silyl triflates was developed. Diverse 2,5-disubstituted tetrazole hemiaminal silyl ethers were obtained with 37?:?63->99?:?1 regioisomeric ratios. The regioselectivities of this reaction were significantly affected by steric hindrance and the conjugation effects of substitutions on the 5-position of tetrazoles.
Green synthetic approach to 5-substituted-1h-tetrazoles via recycle and reuse of tributyltin chloride
Sampath,Reddy, V. Prabhakar,Chakravarthy, A. Kalyan,Reddy, P. Pratap
, p. 393 - 396 (2013/02/22)
A simple, safe and efficient process for the recycle of tributyltin chloride from tributyltin hydroxide is developed and its reuse in the synthesis of 5-substituted-1H-tetrazoles is successfully demonstrated, which paved a way to reduce the toxic tin waste significantly. Recycling of tributyltin chloride is possible over six cycles without loss of its activity.
FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE
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Page/Page column 116-117, (2010/09/18)
The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
CHEMICAL COMPOUNDS
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Page/Page column 100-101, (2010/02/07)
Compounds of the formula (I), or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein -N-HET is, for example, formula (Ic) or (If) wherein R1 is, for example, halogen or a (1-4C)alkyl group which is substituted by one subs