138840-96-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of tricyclic pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one scaffolds as selective BuChE inhibitors
Qiu, Guo-Liang,He, Shao-Sheng,Chen, Shi-Chao,Li, Bo,Wu, Hui-Hui,Zhang, Jing,Tang, Wen-Jian
, p. 1506 - 1515 (2018/10/15)
Based on the structural analysis of tricyclic scaffolds as butyrylcholinesterase (BuChE) inhibitors, a series of pyrazolo[1,5-c][1,3]benzoxazin-5(5H)-one derivatives were designed, synthesized and evaluated for their acetylcholinesterase (AChE) and BuChE inhibitory activity. Compounds with 5-carbonyl and 7- or/and 9-halogen substitutions showed potential BuChE inhibitory activity, among which compounds 6a, 6c and 6g showed the best BuChE inhibition (IC50 = 1.06, 1.63 and 1.63 μM, respectively). The structure–activity relationship showed that the 5-carbonyl and halogen substituents significantly influenced BuChE activity. Compounds 6a and 6g were found nontoxic, lipophilic and exhibited remarkable neuroprotective activity and mixed-type inhibition against BuChE (Ki = 7.46 and 3.09 μM, respectively). Docking studies revealed that compound 6a can be accommodated into BuChE via five hydrogen bonds, one Pi–Sigma interaction and three Pi–Alkyl interactions.
Tetrachloro-o-benzoquinone in Organic Synthesis: A Novel Synthetic Route to Pyrazolobenzoxazines and 5,7-Disubstituted-4-hydroxycoumarins
Nawwar, Galal A. M.
, p. 3139 - 3155 (2007/10/02)
A novel synthesis of dihydropyrazolobenzoxazines and their corresponding pyrazolobenzoxazines utilizing tetrachloro-o-benzoquinone - as a dehydrogenating agent - is described.Also, this simple method of dehydrogenation succeeds in
