Matches in SemOpenAlex for { <https://semopenalex.org/work/W4315491146> ?p ?o ?g. }
Showing items 1 to 85 of
85
with 100 items per page.
- W4315491146 endingPage "193" @default.
- W4315491146 startingPage "182" @default.
- W4315491146 abstract "Abstract: Background: Epilepsy is a deep rooted, partially curable brain illness that affects all individuals irrespective of ages and genders. Despite the discovery of various innovative antiepileptic drugs (AEDs), selectivity and toxicity issues remain. Materials and Methods: A series of (S)-1-(2-(substituted benzylamino)-3-methylbutanoyl)pyrrolidin-2-one analogues (5a-r) were synthesized and evaluated for their anticonvulsant activity. The analogues were screened by two gold standard methods, i.e., electroshock (MES) and chemoshock (scPTZ) seizure tests. In addition, the rotarod method was used to test motor impairment in all synthetic analogues for acute neurotoxicity. The paper also reports ADME prediction of all the 18 synthesized compounds, with each parameter discussed in detail. Furthermore, the GABA-A target protein was used in molecular docking experiments. Results: In the MES model, compounds 5e, 5h, 5k, 5l, 5o, and 5r were identified to be the most effective, while compounds 5j, 5k, 5l, 5o, and 5r were the most active against the scPTZ model. The majority of the synthesized analogues passed the neurotoxicity test, according to the findings. ADME prediction of the compounds exhibited good agreement with the in vivo outcomes. The results of molecular docking showed important interactions with TYR 62, ASN 85, ARG 114, ARG 129, and MET 115 at the active site of GABA-A and the results showed good agreement with in vivo results. Conclusion: The findings of the study indicated some of the compounds possessed excellent anticonvulsant activity without noticeable neurotoxicity. These compounds can be investigated further for the formation of newer/novel anticonvulsant agents. Keywords: Pyrrolidine, Anticonvulsant activity, Molecular Docking, GABA-A, Toxicity, ADME prediction." @default.
- W4315491146 created "2023-01-11" @default.
- W4315491146 creator A5019318227 @default.
- W4315491146 creator A5022388464 @default.
- W4315491146 creator A5023904690 @default.
- W4315491146 creator A5033519696 @default.
- W4315491146 creator A5047284360 @default.
- W4315491146 creator A5067088727 @default.
- W4315491146 creator A5078961893 @default.
- W4315491146 creator A5084356121 @default.
- W4315491146 creator A5085255814 @default.
- W4315491146 date "2023-01-09" @default.
- W4315491146 modified "2023-10-03" @default.
- W4315491146 title "Design, Synthesis and Molecular Docking Studies of (S)-1-(2-(substituted benzylamino)-3- methylbutanoyl)pyrrolidin-2-one analogues as GABA Mediated Anticonvulsant agents" @default.
- W4315491146 doi "https://doi.org/10.5530/001954641726" @default.
- W4315491146 hasPublicationYear "2023" @default.
- W4315491146 type Work @default.
- W4315491146 citedByCount "0" @default.
- W4315491146 crossrefType "journal-article" @default.
- W4315491146 hasAuthorship W4315491146A5019318227 @default.
- W4315491146 hasAuthorship W4315491146A5022388464 @default.
- W4315491146 hasAuthorship W4315491146A5023904690 @default.
- W4315491146 hasAuthorship W4315491146A5033519696 @default.
- W4315491146 hasAuthorship W4315491146A5047284360 @default.
- W4315491146 hasAuthorship W4315491146A5067088727 @default.
- W4315491146 hasAuthorship W4315491146A5078961893 @default.
- W4315491146 hasAuthorship W4315491146A5084356121 @default.
- W4315491146 hasAuthorship W4315491146A5085255814 @default.
- W4315491146 hasBestOaLocation W43154911461 @default.
- W4315491146 hasConcept C118552586 @default.
- W4315491146 hasConcept C150903083 @default.
- W4315491146 hasConcept C159110408 @default.
- W4315491146 hasConcept C178790620 @default.
- W4315491146 hasConcept C185592680 @default.
- W4315491146 hasConcept C202751555 @default.
- W4315491146 hasConcept C207001950 @default.
- W4315491146 hasConcept C2775858608 @default.
- W4315491146 hasConcept C2778186239 @default.
- W4315491146 hasConcept C2779491297 @default.
- W4315491146 hasConcept C29730261 @default.
- W4315491146 hasConcept C41685203 @default.
- W4315491146 hasConcept C55493867 @default.
- W4315491146 hasConcept C69366308 @default.
- W4315491146 hasConcept C71240020 @default.
- W4315491146 hasConcept C71924100 @default.
- W4315491146 hasConcept C86803240 @default.
- W4315491146 hasConcept C98274493 @default.
- W4315491146 hasConceptScore W4315491146C118552586 @default.
- W4315491146 hasConceptScore W4315491146C150903083 @default.
- W4315491146 hasConceptScore W4315491146C159110408 @default.
- W4315491146 hasConceptScore W4315491146C178790620 @default.
- W4315491146 hasConceptScore W4315491146C185592680 @default.
- W4315491146 hasConceptScore W4315491146C202751555 @default.
- W4315491146 hasConceptScore W4315491146C207001950 @default.
- W4315491146 hasConceptScore W4315491146C2775858608 @default.
- W4315491146 hasConceptScore W4315491146C2778186239 @default.
- W4315491146 hasConceptScore W4315491146C2779491297 @default.
- W4315491146 hasConceptScore W4315491146C29730261 @default.
- W4315491146 hasConceptScore W4315491146C41685203 @default.
- W4315491146 hasConceptScore W4315491146C55493867 @default.
- W4315491146 hasConceptScore W4315491146C69366308 @default.
- W4315491146 hasConceptScore W4315491146C71240020 @default.
- W4315491146 hasConceptScore W4315491146C71924100 @default.
- W4315491146 hasConceptScore W4315491146C86803240 @default.
- W4315491146 hasConceptScore W4315491146C98274493 @default.
- W4315491146 hasIssue "1" @default.
- W4315491146 hasLocation W43154911461 @default.
- W4315491146 hasOpenAccess W4315491146 @default.
- W4315491146 hasPrimaryLocation W43154911461 @default.
- W4315491146 hasRelatedWork W1646515875 @default.
- W4315491146 hasRelatedWork W1969461793 @default.
- W4315491146 hasRelatedWork W1991766351 @default.
- W4315491146 hasRelatedWork W2047237283 @default.
- W4315491146 hasRelatedWork W2060064011 @default.
- W4315491146 hasRelatedWork W2079763637 @default.
- W4315491146 hasRelatedWork W2106369820 @default.
- W4315491146 hasRelatedWork W2186970651 @default.
- W4315491146 hasRelatedWork W2411043456 @default.
- W4315491146 hasRelatedWork W4205549877 @default.
- W4315491146 hasVolume "57" @default.
- W4315491146 isParatext "false" @default.
- W4315491146 isRetracted "false" @default.
- W4315491146 workType "article" @default.