81438-56-4Relevant academic research and scientific papers
Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents
Wang, Apeng,Lv, Kai,Li, Linhu,Liu, Hongtao,Tao, Zeyu,Wang, Bin,Liu, Mingliang,Ma, Chao,Ma, Xican,Han, Bing,Wang, Aoyu,Lu, Yu
, p. 715 - 725 (2019/06/24)
A series of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides (IPAs), based on the structure of WZY02 discovered in our lab, were designed and synthesized as new anti-TB agents. Results reveal that many of them exhibit excellent in vitro inhibitory activity with low nanomolar MIC values against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates. Compounds 15b and 15d display good safety and pharmacokinetic profiles, suggesting their promising potential to be lead compounds for future antitubercular drug discovery.
NITROGENOUS HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION THEREOF, AND APPLICATION THEREOF
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, (2019/06/12)
Provided are a nitrogenous heterocyclic aromatic compound, a preparation method therefor, a pharmaceutical composition thereof, and an application thereof. The nitrogenous heterocyclic aromatic compound can be used for treating and/or preventing various diseases mediated by ALK5.
Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
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Page/Page column 344, (2016/04/26)
The present invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
Microwave assisted synthesis of disubstituted imidazo[1,2-a]pyridine-3-carboxylic acid esters
Li, Lin-Hu,Wu, Zhao-Yang,Li, Zhuo-Rong,Liu, Ming-Liang,Guo, Hui-Yuan,Zhang, Qiu-Rong
, p. 2087 - 2096 (2015/12/12)
A novel and efficient synthetic method leveraging microwave-assisted organic synthesis (MAOS) to prepare disubstituted imidazo[1,2-a]- pyridine-3-carboxylic acid esters (IPCEs) (3a-z), the key intermediates for a class of novel anti-tuberculosis agents, is reported. Under microwave heating at 120 °C for 20 or 30 min, the condensations of 2-aminopyridines (1a-k) and ethyl 2-halogenated acetoacetates (2a-d) were conveniently performed in ethanol with acceptable yields.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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Page/Page column 67, (2015/02/19)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase α and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.
COMBINATION OF KINASE INHIBITORS AND USES THEREOF
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Paragraph 00641, (2014/10/04)
The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase a and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3 -kinase α and/or mTOR in a subject.
Thermal and microwave-assisted rapid syntheses of substituted imidazo[1,2-a]pyridines under solvent- and catalyst-free conditions
Chunavala, Kaushik C.,Joshi, Girdhar,Suresh, Eringathodi,Adimurthy, Subbarayappa
experimental part, p. 635 - 641 (2011/04/15)
Thermal and microwave-assisted rapid syntheses of highly substituted imidazo[1,2-a]pyridine derivatives by reaction of aminopyridines and -bromo - keto esters under solvent-free conditions are described. Reactions carried out under microwave irradiation give the highest yields of products in reaction times of less than two minutes. Georg Thieme Verlag Stuttgart New York.
BICYCLIC HETEROARYLS AS KINASE INHIBITORS
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Page/Page column 106-107, (2011/05/06)
The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.
