925920-62-3Relevant articles and documents
Design, synthesis and biological evaluation of selected 3-[3-(amino) propoxy] benzenamines as acetylcholinesterase inhibitors
Malik, Ruchi,Gupta, Richa,Srivastava, Shubham,Choudhary, Bhanwar Singh,Sharma, Manish
, p. 2382 - 2394 (2017/08/16)
The present paper describes design, synthesis, and biological evaluation of a series of some 3-[3-(amino)propoxy]benzenamines as acetylcholinesterase inhibitors using mice as a model and piracetam as a reference drug. The structures of these compounds were confirmed by spectral analysis and compounds were tested for memory enhancing activity using elevated plus maze test and acetylcholinesterase inhibitory assay. The inhibitory range of synthesized compounds was from 8.99 to 28.31?μM. The synthesized compounds possessed higher or equivalent percent retention as compared to piracetam at 1?mg/kg with no other CNS-related activities (locomotor and muscle relaxant, analgesic and anticonvulsant activities). Compound 3-[3-(imidazolo)propoxy]benzenamine has shown significant dose-dependent (1 and 3?mg/kg) memory enhancing activity, while 3-[3-(pyrrolidino)propoxy]benzenamine also showed activity equivalent to reference drug piracetam at 1?mg/kg. Both compounds 3-[3-(pyrrolidino)propoxy]benzenamine and 3-[3-(imidazolo)propoxy]benzenamine were also found to show AChE inhibition with IC50 value of 8.99 and 17.87?μM. The molecular docking, MM-GBSA and molecular dynamics simulation studies were performed in order to establish a relationship between the biological results. RMSD, root-mean-square fluctuations, and interaction patterns of 10a–AChE and Sck–AChE complexes proved that the binding affinity of 10a toward AChE was highly stable with the proposed binding orientations.
IMIDAZO-THIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 181, (2009/07/03)
Compounds of formula I that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. Formula I and therapeutically acceptable salts, prodrugs and salts of prodrugs thereof, wherein X is CH or N; A1 is R1, OR1. NHR1, N(R1)2, NHC(O)R1, NHC(O)NHR1, NHC(O)N(R1)2, NHC(O)OR1, C(O)NHR1, C(O)N(R1)2, C=NOR1, or C(NH2)NOC(O)R1;
SOLUBLE EPOXIDE HYDROLASE INHIBITORS
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Page/Page column 90, (2008/12/07)
Disclosed are urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.
