Yazar "Sarac, Selma" seçeneğine göre listele

Listeleniyor 1 - 2 / 2
  • Küçük Resim Yok
    Öğe
    New Anti-Seizure (Arylalkyl)azole Derivatives: Synthesis, In Vivo and In Silico Studies
    (Wiley-V C H Verlag Gmbh, 2017) Sari, Suat; Dalkara, Sevim; Kaynak, Filiz Betul; Reynisson, Johannes; Sarac, Selma; Karakurt, Arzu
    (Arylalkyl)azoles are a class of antiepileptic compounds including nafimidone, denzimol, and loreclezole (LRZ). Nafimidone and denzimol are thought to inhibit voltage-gated sodium channels (VGSCs) and enhance -aminobutyric acid (GABA)-mediated response. LRZ, a positive allosteric modulator of A-type GABA receptors (GABA(A)Rs), was reported to be sensitive to Asn265 of the 2/3 subunit. Here, we report new N-[1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene]hydroxylamine esters showing anticonvulsant activity in animal models, including the 6-Hz psychomotor seizure test, a model for therapy-resistant partial seizure. We performed molecular docking studies for our active compounds using GABA(A)R and VGSC homology models. They predicted high affinity to the benzodiazepine binding site of GABA(A)R in line with the experimental results. Also, the binding mode and interactions of LRZ in its putative allosteric binding site of GABA(A)R is elucidated.
  • Küçük Resim Yok
    Öğe
    Synthesis, anticonvulsant activity, and molecular modeling studies of novel 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol ester derivatives
    (Springer Birkhauser, 2018) Dogan, Inci Selin; Ozdemir, Zeynep; Sari, Suat; Bozbey, Irem; Karakurt, Arzu; Sarac, Selma
    A series of new ester derivatives were synthesized by the reaction of various acids with 1-phenyl/1-(4-chlorophenyl)-2-(1H-triazol-1-yl)ethanol and in vivo screened for their anticonvulsant activity. The title compounds were screened against MES and ScM seizure tests according to a modified version of the Epilepsy Therapy Screening Program (ETSP) protocol of the National Institutes of Health (NIH). Their neurotoxic effects were evaluated by the rotarod test. All the compounds showed protection against MES and/or ScM-induced seizures at 30 mg/kg without neurotoxicity. More compounds were found active in the ScM test and at lower dose than the MES test. Physicochemical and pharmacokinetic profiles of the compounds were predicted by QikProp. Using molecular docking approach we tried to get insights into their possible anticonvulsant mechanisms.