1524-19-2Relevant academic research and scientific papers
Method for selectively preparing hydroquinone monoether compound or quinol compound (by machine translation)
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Paragraph 0034-0039; 0050-0052; 0057-0058, (2020/12/30)
The method comprises the following steps: taking an organic boric acid compound and a p-benzoquinone compound as a reaction raw material, under the action of a copper catalyst, selectively reacting to obtain a hydroquinone monoether compound or a quinol compound. Compared with the prior art, the method disclosed by the invention adopts a one-pot reaction, can selectively obtain two products through solvent control, is suitable for preparing various types of hydroquinone monoether compounds and quinol compounds, and has wide applicability. The substrate functional group is high in tolerance and wide in substrate range. The raw material and the catalyst are cheap and easily available, the reaction conditions are mild, the reaction solvent is green and environment-friendly, the post-treatment is simple, and the yield and purity of the product are high. The preparation method is convenient. The method is rapid and efficient, and has a good application prospect in drug molecule synthesis. (by machine translation)
Quinoline derivative as well as preparation method and application thereof (by machine translation)
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Paragraph 0261; 0263-0267, (2019/11/28)
The invention provides a quinoline derivative and a composition containing the same. The invention also provides a method for preparing the derivative and application of the derivative and the composition to kill pests. (by machine translation)
Synthesis and biological evaluation of XB-1 analogues as novel histamine H3 receptor antagonists and neuroprotective agents
Bao, Xiaofeng,Jin, Yanyan,Liu, Xiaolu,Liao, Hong,Zhang, Luyong,Pang, Tao
, p. 6761 - 6775 (2014/02/14)
A novel class of H3 receptor antagonists, XB-1 analogues based on benzophenone or oxydibenzene scaffolds were synthesized, and their biological activities were evaluated to determine their in vitro neuroprotective effects against Aβ25-35-induced damage in primary cortical neurons and against glutamate-induced neuronal injury in primary cerebellar granule neurons. The results indicated that all of the tested analogues displayed neuroprotective activity at 0.1 μM or 1 μM. These findings may provide new insights into the development of novel promising H3 receptor antagonists with potential neuroprotective activity.
Fluorine-containing aryloxyethyl thiocyanate derivatives are potent inhibitors of Trypanosoma cruzi and Toxoplasma gondii proliferation
Linares, Guadalupe Garcia,Gismondi, Santiago,Codesido, Nicolas Osa,Moreno, Silvia N.J.,Docampo, Roberto,Rodriguez, Juan B.
, p. 5068 - 5071 (2008/03/13)
As a part of our project aimed at developing new safe chemotherapeutic and chemoprophylactic agents against tropical diseases, fluorine-containing drugs structurally related to 4-phenoxyphenoxyethyl thiocyanate (1) were designed, synthesized, and evaluate
Selective displacement of aryl fluorides with hydroquinone: Synthesis of 4-phenoxyphenols
Marcune, Benjamin F.,Hillier, Michael C.,Marcoux, Jean-Fran?ois,Humphrey, Guy R.
, p. 7823 - 7826 (2007/10/03)
The selective displacement of a variety of aryl fluorides with hydroquinone has been achieved to give substituted 4-phenoxyphenols 3. In some cases the addition of 18-crown-6 resulted in a significant rate enhancement, and the reactions could be carried out at lower temperature. One of these derivatives, 3a (X = Cl) was converted to 2-propyl-4-(4-chlorophenoxy)phenol 2a, a precursor to the PPARγ receptor agonist 1.
(2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents
Koyama, Hiroo,Boueres, Julia K.,Miller, Daniel J.,Berger, Joel P.,MacNaul, Karen L.,Wang, Pei-Ran,Ippolito, Marc C.,Wright, Samuel D.,Agrawal, Arun K.,Moller, David E.,Sahoo, Soumya P.
, p. 3347 - 3351 (2007/10/03)
A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
5-Aryl thiazolidine-2,4-diones as selective PPARγ agonists
Koyama, Hiroo,Boueres, Julia K.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,Miller, Daniel J.,Tolman, Richard L.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 1801 - 1804 (2007/10/03)
A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.
5-Aryl thiazolidine-2,4-diones: Discovery of PPAR dual α/γ agonists as antidiabetic agents
Desai, Ranjit C.,Han, Wei,Metzger, Edward J.,Bergman, Jeffrey P.,Gratale, Dominick F.,MacNaul, Karen L.,Berger, Joel P.,Doebber, Thomas W.,Leung, Kwan,Moller, David E.,Heck, James V.,Sahoo, Soumya P.
, p. 2795 - 2798 (2007/10/03)
A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARα/γ agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.
LTA4 Hydrolase inhibitors
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Page 59, (2010/01/31)
The present invention provides compounds of the formula Ar1-Q-Ar2-Y-R-Z and pharmaceutically acceptable salts thereof wherein Ar1 and Ar2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as proriasis, ulcerative colitis, IBD and asthma.
Antidiabetic agents
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, (2008/06/13)
The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and related diseases and for lowering triglyceride levels are also disclosed.
