“…1) Since the anticonvulsant agents currently used in the treatment of epilepsy have certain disadvantages such as notable side effects and inefficient therapy in some seizure types, a clear need for safer and more effective antiepileptic drugs is well known. [1][2][3] Therefore the development of new antiepileptic drugs with approved therapeutic properties is an important challenge for medicinal chemists.…”
؊1 and 13, respectively. The PI value of compound 4g was better than that of most marketed drugs. Structure-activity relationships are also described in this paper.
“…1) Since the anticonvulsant agents currently used in the treatment of epilepsy have certain disadvantages such as notable side effects and inefficient therapy in some seizure types, a clear need for safer and more effective antiepileptic drugs is well known. [1][2][3] Therefore the development of new antiepileptic drugs with approved therapeutic properties is an important challenge for medicinal chemists.…”
؊1 and 13, respectively. The PI value of compound 4g was better than that of most marketed drugs. Structure-activity relationships are also described in this paper.
“…Nevertheless, approximately 30% of the patients don't repay to the available antiepileptic medications [3]. In addition, long term administration of the currently used antiepileptics is accompanied by unfavourable side effects like megaloblastic anaemia and hepatotoxicity [4,5]. Accordingly, the search for new antiepileptic agents endowed with high potency and better safety profile has gained a considerable attention.…”
CCDC no.: 1507255The crystal structure is shown in the figure. Tables 1 and 2 contain details on crystal structure and measurement conditions and a list of the atoms including atomic coordinates and displacement parameters.
Source of materialTo a solution of 1-(chloroacetyl)-2,3-diphenyl-1,3-diazaspiro [4.5]decan-4-one (1.8 g, 0.0047 mol) in toluene (40 mL) was added morpholine (2.0 g, 0.023 mol). The mixture was heated at 90°C overnight, cooled to room temperature and solvent was evaporated under reduced pressure. The obtained buff solid was dissolved in methylene chloride (100 mL) and washed two times with water. The organic phase was separated, dried (Na 2 SO4) and evaporated under vacuum to furnish the title compound as a white solid. The crude product was re-crystallized from a mixture of petroleum ether (40-60) and ethyl acetate to afford white crystals (m.p. 441-443 K) in 60% yield [1]. Crystals were obtained by slow evaporation of its ethyl acetate solution.
“…Many new antiepileptic drugs have been introduced in the market, however the available antiepileptics fail to prevent the seizures in approximately 30% of patients [6]. Moreover, these medications are associated with severe adverse effects such as gingival hyperplasia, megaloblastic anaemia and hepatotoxicity [7,8]. Therefore, there is a great need for the development of new, more effective and less toxic antiepileptic agents.…”
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