29775-73-3Relevant articles and documents
Theoretical molecular properties prediction, docking and antimicrobial studies on Anisidine-Isatin Schiff bases
Ayyadurai, G. K.,Jayaprakash, R.,Rathika, S.
, p. 3025 - 3030 (2021/12/14)
The continuous intake of a specific antibiotic for diseases is continuously reducing the immunity of the human in course of time, which includes Covid-19 treatment. Recent research on Schiff bases shows the promising biological activities and good antibac
Design, synthesis and biological activity of novel tacrine-isatin Schiff base hybrid derivatives
Riazimontazer,Sadeghpour,Nadri,Sakhteman,Tüylü Kü?ükk?l?n?,Miri,Edraki
, (2019/06/05)
A series of novel tacrine-isatin Schiff base hybrid derivatives (7a-p)were designed, synthesized and evaluated as multi-target candidates against Alzheimer's disease (AD). The biological assays indicated that most of these compounds displayed potent inhibitory activity toward acetylcholinesterase (AChE)and butyrylcholinesterase (BuChE)and specific selectivity for AChE over BuChE. It was also found that they act as excellent metal chelators. The compounds 7k and 7m were found to be good inhibitors of AChE-induced amyloid-beta (Aβ)aggregation. Most of the compounds inhibited AChE with the IC50 values, ranging from 0.42 nM to 79.66 nM. Amongst them, 7k, 7m and 7p, all with a 6 carbon linker between tacrine and isatin Schiff base exhibited the strongest inhibitory activity against AChE with IC50 values of 0.42 nM, 0.62 nM and 0.95 nM, respectively. They were 92-, 62- and 41-fold more active than tacrine (IC50 = 38.72 nM)toward AChE. Most of the compounds also showed a potent BuChE inhibition among which 7d with an IC50 value of 0.11 nM for BuChE is the most potent one (56-fold more potent than that of tacrine (IC50 = 6.21 nM)). In addition, most compounds exhibited the highest metal chelating property. Kinetic and molecular modeling studies revealed that 7k is a mixed-type inhibitor, capable of binding to catalytic and peripheral site of AChE. Our findings make this hybrid scaffold an excellent candidate to modify current drugs in treating Alzheimer's disease (AD).
Microwave-assisted synthesis and evaluation of indole derivatives as potential anthelmintic agents
Panda, Jnyanaranjan,Kumar, Anjan,Sahoo, Biswa Mohan,Banik, Bimal Krishna
, p. 1283 - 1288 (2020/06/27)
An efficient method is developed and exploited for the synthesis of indole derivatives via microwave-assisted technology. By considering the advantage microwave synthesis in terms of high efficient energy, indole derivatives are prepared. In the current study, the Schiff's bases are first synthesized by reaction of 1H-indole-2,3-dione (isatin) with various substituted anilines in presence of acetic acid under microwave irradiation. Then the Mannich bases are produced by condensation of Schiff bases with different secondary amines in the presence of formaldehyde. The newly synthesized compounds are characterized by TLC report and spectral data followed by evaluation for anthelmintic activity against Pheretima posthuma. Albendazole is used as standard drug for comparative study. The titled compounds are screened for anthelmintic activity at the concentration of 10, 20 and 50 mg/ml. The anthelmintic effect of standard drug Albendazole is also evaluated at 10 mg/ml. The results of present study indicate that some of the tested compounds exhibit significant anthelmintic activity in dose dependent manner.
