Abulkhair, Hamada S. published the artcileIn vivo- and in silico-driven identification of novel synthetic quinoxalines as anticonvulsants and AMPA inhibitors, Recommanded Product: 2-Chloroacetamide, the publication is Archiv der Pharmazie (Weinheim, Germany) (2021), 354(5), 2000449, database is CAplus and MEDLINE.
The lack of effective therapies for epileptic patients and the potentially harmful consequences of untreated seizure incidents have made epileptic disorders in humans a major health concern. Therefore, new and more potent anticonvulsant drugs are continually sought after, to combat epilepsy. On the basis of the pharmacophoric structural specifications of effective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists with an efficient anticonvulsant activity, the present work reports the design and synthesis of two novel sets of quinoxaline derivatives The anticonvulsant activity of the synthesized compounds was evaluated in vivo according to the pentylenetetrazol-induced seizure protocol, and the results were compared with those of perampanel as a reference drug. Among the synthesized compounds, four showed promising activities with ED50 values of 37.50, 23.02, 29.16, and 23.86 mg/kg. Docking studies of these compounds suggested that AMPA binding could be the mechanism of action of these derivatives Overall, the pharmacophore-based structural optimization, in vivo and in silico docking, and druglikeness studies indicated that the designed compounds could serve as promising candidates for the development of effective anticonvulsant agents with good pharmacokinetic profiles.
Archiv der Pharmazie (Weinheim, Germany) published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Recommanded Product: 2-Chloroacetamide.
Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics