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Synthesis, biological and computational evaluation of benzoxazole hybrid analogs as potential anti-Alzheimer's agents.
Othman, Mohamed S; Hussain, Rafaqat; Rahim, Fazal; Ullah, Hayat; Khan, Shoaib; Taha, Muhammad; Fareid, Mohamed A; Altaleb, Anas T; Aboelnaga, Shimaa M; Shah, Syed Adnan Ali.
Afiliación
  • Othman MS; Biochemistry Department, College of Medicine, University of Ha'il, Hail, 2440, Saudi Arabia.
  • Hussain R; Faculty of Biotechnology, October University for Modern Science & Arts (MSA), Giza, Egypt.
  • Rahim F; Department of Chemistry, Hazara University, Mansehra, 21120, Pakistan.
  • Ullah H; Department of Chemistry, Hazara University, Mansehra, 21120, Pakistan.
  • Khan S; Institute of Chemistry, University of Okara, Okara- 56300, Pakistan.
  • Taha M; Department of Chemistry, Abbottabad University of Science & Technology (AUST), Abbottabad, Pakistan.
  • Fareid MA; Department of Clinical Pharmacy, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam, 31441, Saudi Arabia.
  • Altaleb AT; Department of Medical Laboratories, Faculty of Applied Medical Science, University of Ha'il, Hail, 2440, Saudi Arabia.
  • Aboelnaga SM; Botany & Microbiology Department, Faculty of Science, Al-Azhar University, Cairo, 11651, Egypt.
  • Shah SAA; Basic Sciences Department, Deanship of Preparatory Year, University of Ha'il, Hail, 2440, Saudi Arabia.
Future Med Chem ; 16(19): 2013-2023, 2024.
Article en En | MEDLINE | ID: mdl-39269160
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 IC50 values 1.10 ± 0.40-24.50 ± 0.90 µM against acetylcholinesterase (AChE) and 1.90 ± 0.70-28.60 ± 0.60 µM 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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Benzoxazoles / Butirilcolinesterasa / Inhibidores de la Colinesterasa / Enfermedad de Alzheimer / Simulación del Acoplamiento Molecular Límite: Humans Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Acetilcolinesterasa / Benzoxazoles / Butirilcolinesterasa / Inhibidores de la Colinesterasa / Enfermedad de Alzheimer / Simulación del Acoplamiento Molecular Límite: Humans Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Reino Unido