152121-41-0Relevant academic research and scientific papers
The anion of 3-methyl-2-pyridin-4-yl-1,3-oxazine
Sheldrake, Peter,Tyrrell, Elizabeth,Mintias, Shirin,Shahid, Imran
, p. 2263 - 2268 (2003)
n-Butyllithium at -78°C readily abstracts the methine proton from the title compound. The anion reacts efficiently with a range of electrophiles to provide 4-pyridyl ketones upon acid hydrolysis.
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38α mitogen-activated protein kinase inhibitors
Koch, Pierre,Jahns, Hartmut,Schattel, Verena,Goettert, Marcia,Laufer, Stefan
supporting information; experimental part, p. 1128 - 1137 (2010/08/05)
Various substituted 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4-yl)quinoxalines and 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4-yl)pyridopyrazines were synthesized as novel p38α MAP kinase inhibitors via different short synthetic strategies with high variation possibilities. The formation of the quinoxaline/ pyridopyrazine core was achieved from α-diketones and o-phenylenediamines/ α-diaminopyridines under microwave irradiation. Introduction of an amino moiety at the pyridine C2 position of the 2(3)-(4-fluorophenyl)-3(2)-(pyridin-4- yl)quinoxalines led to compounds showing potent enzyme inhibition down to the double-digit nanomolar range (6f; IC50 = 81 nM). Replacement of the quinoxaline core with pyrido[2,3-b]pyrazine gave compound 9e with superior p38α MAP kinase inhibition (IC50= 38 nM).
Role of the hydrogen bonding heteroatom-lys53 interaction between the p38r mitogen-activated protein (map) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors
Thaher, Bassam Abu,Koch, Pierre,Schattel, Verena,Laufer, Stefan
supporting information; experimental part, p. 2613 - 2617 (2010/02/28)
In the framework of investigating the role of heteroatoms in pyridinyl-substituted 5-membered (hetero)cycles as potential p38α MAP kinase inhibitor scaffolds, cyclopentene, pyrrole, furan, and imidazole analogues were synthesized and tested with respect t
PYRAZINE DERIVATIVES USEFUL AS ADENOSINE RECEPTOR ANTAGONISTS
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Page/Page column 58-59, (2008/06/13)
The present invention provides a compound of formula (I) wherein: A represents an optionally substituted monocyclic or polycyclic aryl or heteroaryl group B represents an optionally substituted monocyclic nitrogen-containing heteroaryl group ; and either a) R1 and R2 represent hydrogen or specified substituents, or b) R2, R1 and the -NH- group to which R1 is attached, form a moiety selected from the moiety of formulae (IIa) and (IIb): (IIa) These compounds are useful as antagonists of the A2B receptor, for instance in the treatment of asthma.
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
Biftu, Tesfaye,Feng, Dennis,Ponpipom, Mitree,Girotra, Narindar,Liang, Gui-Bai,Qian, Xiaoxia,Bugianesi, Robert,Simeone, Joseph,Chang, Linda,Gurnett, Anne,Liberator, Paul,Dulski, Paula,Leavitt, Penny Sue,Crumley, Tami,Misura, Andrew,Murphy, Terence,Rattray, Sandra,Samaras, Samantha,Tamas, Tamas,Mathew, John,Brown, Christine,Thompson, Don,Schmatz, Dennis,Fisher, Michael,Wyvratt, Matthew
, p. 3296 - 3301 (2007/10/03)
Several analogs of 2,3-diaryl pyrroles were synthesized and evaluated as inhibitors of Eimeria tenella cGMP-dependent protein kinase and in in vivo anticoccidial assays. A 4-fluorophenyl group enhances both in vitro and in vivo activities. The most potent
Imidazolyl-cyclic acetals
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, (2008/06/13)
Compounds of formula (I) are described in which R1is optionally substituted heteroaryl; R2is optionally substituted aryl or optionally substituted heteroaryl; R3is a group —L1—R7or —L2—Rsu
2-substituted imidazoles useful in the treatment of inflammatory diseases
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, (2008/06/13)
This invention relates to substituted imidazoles of Formula I pharmaceutical compositions containing them, methods of using them and intermediates useful in their manufacture. The compounds of the invention modulate the production of a number of inflammat
Substituted imidazoles useful in the treatment of inflammatory disease
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, (2008/06/13)
This invention relates to a series of substituted imidazoles of Formula I STR1 pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention inhibit the production of a number of inflammatory cytok
