30611-21-3Relevant articles and documents
Design, synthesis, and effects of novel phenylpyrimidines as glucagon receptor antagonists
Choi, Hojung,Lee, Chang-Yong,Park, Eun-Young,Lee, Kyoung Mee,Shin, Dongyun,Jun, Hee-Sook
, p. 5701 - 5710 (2018)
The hormone glucagon increases blood glucose levels through increasing hepatic glucose output. In diabetic patients, dysregulation of glucagon secretion contributes to hyperglycemia. Thus, the inhibition of glucagon receptor is one target for the treatment of hyperglycemia in type 2 diabetes. Here we designed and synthesized a series of small molecules based on phenylpyrimidine. Of these, the compound (R)-7a most significantly decreased the glucagon-induced cAMP production and glucagon-induced glucose production during in vitro and in vivo assays. In addition, (R)-7a showed good efficacy in glucagon challenge tests and lowered blood glucose levels in diabetic db/db mice. Our results suggest that the compound (R)-7a could be a potential glucose-lowering agent for treating type 2 diabetes.
A phenylpyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating Glucagon Receptor activity related diseases containing the same as an active ingredient
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Paragraph 0207-0210, (2020/04/29)
The present invention relates to a phenylpyrimidine derivative, a method for manufacturing the same, and a pharmaceutical composition for preventing or treating glucagon receptor activity- related diseases. It is confirmed that the phenylpyrimidine deriva
Synthesis of Functionalized Ketones from Acid Chlorides and Organolithiums by Extremely Fast Micromixing
Nagaki, Aiichiro,Sasatsuki, Kengo,Ishiuchi, Satoshi,Miuchi, Nobuyuki,Takumi, Masahiro,Yoshida, Jun-ichi
supporting information, p. 4946 - 4950 (2019/03/21)
Synthesis of ketones containing various functional groups from acid chlorides bearing electrophilic functional groups and functionalized organolithiums was achieved using a flow microreactor system. Extremely fast mixing is important for high chemoselectivity.
AMIDE COMPOUNDS AND USE THEREOF
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Page/Page column 73; 74, (2018/08/20)
Disclosed are compounds of formula (I) below and pharmaceutically acceptable salts thereof, in which each of variables R1, R2, L, and Z is defined herein. Also disclosed are methods for reducing the glycemic level and treating glucag
Rhodium-catalyzed allyl transfer from homoallyl alcohols to aldehydes via retro-allylation followed by isomerization into ketones
Takada, Yuko,Hayashi, Sayuri,Hirano, Koji,Yorimitsu, Hideki,Oshima, Koichiro
, p. 2515 - 2517 (2007/10/03)
Retro-allylation of homoallyl alcohol by rhodium catalysis occurs to generate allylrhodium species. This allylrhodium reacts with aldehydes to give the corresponding secondary alcohols in situ. Isomerization of these alcohols proceeds in the same pots to furnish the corresponding saturated ketones in good yields.
Deactivation of Triplet Phenyl Alkyl Ketones by Conjugatively Electron-Withdrawing Substituents
Wagner, Peter J.,Siebert, Elizabeth J.
, p. 7329 - 7335 (2007/10/02)
Para-cyano, -carbomethoxy, and -acyl substituents decrease the triplet reactivity of valerophenone (γ-hydrogen abstraction), whereas comparable meta substituents increase reactivity.Spectroscopic results are presented which indicate that para-(-R) substituents lower ?,?* triplet energies so much more than n,?* energies that the lowest triplets become largely ?,?* in nature.Meta-(-R) substituents do not stabilize ?,?* triplets enough to invert triplet levels.Both substitution patterns support a largely 1,4-biradical structure for the lowest ?,?* triplet of acylbenzenes.Ortho substituents show the usual steric anomalies: ortho cyano enhances valerophenone triplet reactivity by stabilizing the n,?* triplet; ortho carbomethoxy deactivates valerophenone by stabilizing the ?,?* triplet but not the n,?.*