39497-01-3Relevant academic research and scientific papers
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit
Cushing, Timothy D.,Baichwal, Vijay,Berry, Karen,Billedeau, Roland,Bordunov, Viola,Broka, Chris,Cardozo, Mario,Cheng, Peng,Clark, David,Dalrymple, Stacie,Degraffenreid, Michael,Gill, Adrian,Hao, Xiaolin,Hawley, Ronald C.,He, Xiao,Jaen, Juan C.,Labadie, Sharada S.,Labelle, Marc,Lehel, Csaba,Lu, Pu-Ping,McIntosh, Joel,Miao, Shichang,Parast, Camran,Shin, Youngsook,Sjogren, Eric B.,Smith, Marie-Louise,Talamas, Francisco X.,Tonn, George,Walker, Keith M.,Walker, Nigel P.C.,Wesche, Holger,Whitehead, Chris,Wright, Matt,Browner, Michelle F.
, p. 417 - 422 (2011)
A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our early efforts at optimization of the quinoline core, the imidazole and the semithiocarbazone moiety. Most potency gains came from substitution around the 6- and 7-positions of the quinoline ring. Replacement of the semithiocarbazone with a semicarbazone decreased potency but led to some measurable exposure.
A novel method for heterocyclic amide-thioamide transformations
Fathalla, Walid,Ali, Ibrahim A. I.,Pazdera, Pavel
, p. 174 - 181 (2017/02/15)
In this paper, we introduce a novel and convenient method for the transformation of heterocyclic amides into heteocyclic thioamides. A two-step approach was applied for this transformation: Firstly, we applied a chlorination of the heterocyclic amides to afford the corresponding chloroheterocycles. Secondly, the chloroherocycles and N-cyclohexyl dithiocarbamate cyclohexylammonium salt were heated in chloroform for 12 h at 61°C to afford heteocyclic thioamides in excellent yields.
Design, synthesis and evaluation of a new calix[4]arene based molecular receptor for multiple ion selectivity
Chawla, Har Mohindra,Gupta, Tanu
, p. 49 - 56 (2015/04/22)
The hydrophobic and conformational motifs of calix[4]arene stereostructure and plausible binding characteristics of heterocyclic 2-oxo-1,2-dihydroquinoline-4-carbohydrazide have been deployed for the design and synthesis of a new molecular receptor, 4 for multi-ion recognition. The target molecule was synthesized through the condensation of 3 with 2-oxo-1,2-dihydroquinoline-4-carbohydrazide (6) in refluxing ethanol. It has been determined that 4 exhibits an exclusive color change from colorless to yellow as well as a 5.5 fold increase in the fluorescence intensity upon interaction with fluoride due to formation of multiple hydrogen bonds. Consequent to fluoride induced deprotonation, 4 displays a dual selectivity for Cu2+ and Ni2+ ions from amongst plethora of investigated cations.
Microwave-assisted synthesis of 3,1-benzoxazin-2-ones from 3-hydroxyoxindoles
Suarez-Castillo, Oscar R.,Bautista-Hernandez, Claudia I.,Sanchez-Zavala, Maricruz,Melendez-Rodriguez, Myriam,Sierra-Zenteno, Araceli,Morales-Rios, Martha S.,Joseph-Nathan, Pedro
, p. 2147 - 2171,25 (2020/08/31)
A general protocol for the synthesis of 3,1-benzoxazin-2-ones 18 from 3-hydroxyoxindoles 16 in a two steps sequence through phenylsuccinates or phenylpropionates 17 is described. Best reaction conditions for ring opening of 16 to succinates or propionates 17 were achieved using alcohol/silica gel, while cyclization of 17 to benzoxazinones 18 was easily done with HCl/alcohol. It was also found that 17 and 18 can be transesterified using HCl/alcohol. Most transformations were carried out by traditional heating and by microwave (MW) irradiation to accelerate reaction rates.
COMPOUNDS FOR THE INHIBITION OF CELLULAR PROLIFERATION
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Page/Page column 64-65, (2012/02/01)
Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.
Heteroaromatic tosylates as electrophiles in regioselective Mizoroki-Heck-coupling reactions with electron-rich olefins
Gogsig, Thomas M.,Lindhardt, Anders T.,Dekhane, Mouloud,Grouleff, Julie,Skrydstrup, Troels
supporting information; experimental part, p. 5950 - 5955 (2010/02/28)
Heteroaromatic 2-pyridyl tosylates were successfully applied as electrophiles in palladium(0)-catalyzed Mizoroki-Heck-coupling reactions to electron-rich olefins with complete aregioselectivity. This protocol represents a general strategy for the application of pyridyl tosylates and mesylates in the Mizoroki-Heck coupling. The catalytic system also proved adaptable to changes in the heteroaromatic core as well as large-scale applications. Finally, the synthetic utility of the functionalized α-heteroarylvinyl amides was established providing straightforward access to highly functionalized heteroaromatic compounds including chiral benzylic amide derivatives.
RENIN INHIBITORS
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Page/Page column 40, (2008/06/13)
The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
NOVEL CYANOGUANIDINE COMPOUNDS
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Page/Page column 19, (2008/06/13)
Novel pyridyl cyanoguanidien compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neoplastic diseases.
Antiinflammation agents
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, (2008/06/13)
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.
Use of imidazo?1,5-a!quinolones as neuroprotective agents
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, (2008/06/13)
The imidazo?1,5-a!quinolines (I) are useful in treating neurological diseases/conditions or chronic neurodegenerative diseases/conditions.
