| Title : Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents - Othman_2024_Future.Med.Chem__1 |
| Author(s) : Othman MS , Hussain R , Rahim F , Ullah H , Khan S , Taha M , Fareid MA , Altaleb AT , Aboelnaga SM , Ali Shah SA |
| Ref : Future Med Chem , :1 , 2024 |
|
Abstract :
Aim: Current study aims exploration of bis-benzoxazole bearing bis-Schiff base scaffolds (1-16) as anti-Alzheimer's agents.Materials & methods: 2-aminophenol is used as starting materials which react with different reagents in different step to give us bis-benzoxazole bearing bis-Schiff base analogs. NMR and HREI-MS techniques were used for characterization. All derivatives demonstrated varied range of activities with IC(50) values 1.10 +/- 0.40-24.50 +/- 0.90 microM against acetylcholinesterase (AChE) and 1.90 +/- 0.70-28.60 +/- 0.60 microM against butyrylcholinesterase (BuChE) in contrast to donepezil. In both cases, analog-3 was found most potent. Molecular docking explored modes of interactions between scaffolds and receptor sites of targeted enzymes.Conclusion: This study offering promising approach for optimization and development of potent inhibitors of cholinesterase enzymes. |
| PubMedSearch : Othman_2024_Future.Med.Chem__1 |
| PubMedID: 39269160 |
Othman MS, Hussain R, Rahim F, Ullah H, Khan S, Taha M, Fareid MA, Altaleb AT, Aboelnaga SM, Ali Shah SA (2024)
Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents
Future Med Chem
:1
Othman MS, Hussain R, Rahim F, Ullah H, Khan S, Taha M, Fareid MA, Altaleb AT, Aboelnaga SM, Ali Shah SA (2024)
Future Med Chem
:1