55432-58-1Relevant articles and documents
STING AGONISTS AND USES THEREOF
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Paragraph 00615, (2020/07/14)
The present invention provides compounds, compositions thereof, and methods of using the same for the modulation of STING, and the treatment of STING-mediated disorders.
Imidoyl dichlorides as new reagents for the rapid formation of 2-aminobenzimidazoles and related azoles
Pollock, Julie A.,Kim, Sung Hoon,Katzenellenbogen, John A.
, p. 6097 - 6099 (2015/10/28)
The development of a reagent for the efficient synthesis of five- and six-membered azoles at room temperature is proposed. A variety of substituted 2-aminobenzimidazoles are synthesized in good to excellent yields. The ability to incorporate various protecting groups makes the imidoyl dichloride reagent amenable to a large number of syntheses. The reagent is applied to the total synthesis of the 2-aminobenzimidazole containing carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), from 2-chloro-3-nitropyridine in >60% yield in 6 steps.
Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis
Kanhed, Ashish M.,Sinha, Anshuman,Machhi, Jatin,Tripathi, Ashutosh,Parikh, Zalak S.,Pillai, Prakash P.,Giridhar, Rajani,Yadav, Mange Ram
, p. 7 - 12 (2015/06/08)
This article describes discovery of a novel and new class of cholinesterase inhibitors as potential therapeutics for Alzheimer's disease. A series of novel isoalloxazine derivatives were synthesized and biologically evaluated for their potential inhibitory outcome for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds exhibited high activity against both the enzymes AChE as well as BuChE. Of the synthesized compounds, the most potent isoalloxazine derivatives (7m and 7q) showed IC50 values of 4.72 μM and 5.22 μM respectively against AChE; and, 6.98 μM and 5.29 μM respectively against BuChE. These two compounds were further evaluated for their anti-aggregatory activity for β-amyloid (Aβ) in presence and absence of AChE by performing Thioflavin-T (ThT) assay and Congo red (CR) binding assay. In order to evaluate cytotoxic profile of these two potential compounds, cell viability assay of SH-SY5Y human neuroblastoma cells was performed. Further, to understand the binding behavior of these two compounds with AChE and BuChE enzymes, docking studies have been reported.
