384847-18-1Relevant articles and documents
Thieno[2,3-b]pyridine amines: Synthesis and evaluation of tacrine analogs against biological activities related to Alzheimer's disease
Saeedi, Mina,Safavi, Maliheh,Allahabadi, Emad,Rastegari, Arezoo,Hariri, Roshanak,Jafari, Sanaz,Bukhari, Syed N. A.,Mirfazli, Seyedeh S.,Firuzi, Omidreza,Edraki, Najmeh,Mahdavi, Mohammad,Akbarzadeh, Tahmineh
, (2020/07/15)
In search of safer tacrine analogs, various thieno[2,3-b]pyridine amine derivatives were synthesized and evaluated for their inhibitory activity against cholinesterases (ChEs). Among the synthesized compounds, compounds 5e and 5d showed the highest activity towards acetylcholinesterase and butyrylcholinesterase, with IC50 values of 1.55 and 0.23 μM, respectively. The most active ChE inhibitors (5e and 5d) were also candidates for further complementary assays, such as kinetic and molecular docking studies as well as studies on inhibitory activity towards amyloid-beta?(βA) aggregation and β-secretase 1, neuroprotectivity, and cytotoxicity against HepG2 cells. Our results indicated efficient anti-Alzheimer's activity of the synthesized compounds.
An innovative synthesis of tertiary hydroxyl thieno[2,3-d]pyrimidinone skeleton: Natural-like product from the tandem reaction of o-aminothienonitrile and carbonyl compound
Yang, Junjuan,Shi, Daxin,Hao, Pengfei,Yang, Deli,Zhang, Qi,Li, Jiarong
, p. 2455 - 2461 (2016/05/19)
A straightforward base accelerant tandem protocol for the synthesis of the tertiary hydroxyl natural-like thieno[2,3-d]pyrimidinone skeleton was developed from the cyclocondensation of o-aminothienonitrile and carbonyl compound. The reaction process includes PDF conversion and photo-catalytic oxygenation. This synthetic strategy offers an alternative method for regioselective construction of tertiary hydroxylated thieno[2,3-d]pyrimidinone architectures with kinetic, thermodynamic control, and six-member ring effect.
NOVEL THIENOPYRIDINES AS PHARMACOLOGICALLY ACTIVE AGENTS
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Page/Page column 14, (2011/11/12)
The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF-α activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided are compounds of formula (I).
THIENOPYRIDINES AS PHARMACOLOGICALLY ACTIVE AGENTS
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Page/Page column 42-43, (2010/08/04)
The present invention provides compounds and pharmaceutically acceptable salts thereof methods for synthesizing thienopyridines and methods for inhibiting TNF- α activity for the treatment of cancer, asthma, arthritis, diabetes and inflammation. Provided- are compounds of formula (I).