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Highly functionalized 2-amino-4H-pyrans as potent cholinesterase inhibitors.
Kumar, Raju Suresh; Almansour, Abdulrahman I; Arumugam, Natarajan; Al-Thamili, Dhaifallah M; Basiri, Alireza; Kotresha, D; Manohar, Thota Sai; Venketesh, S; Asad, Mohammad; Asiri, Abdullah M.
Afiliação
  • Kumar RS; Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia. Electronic address: sraju@ksu.edu.sa.
  • Almansour AI; Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Arumugam N; Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Al-Thamili DM; Department of Chemistry, College of Sciences, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Basiri A; Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198, United States.
  • Kotresha D; Department of Microbiology, East West Group of Institution, no. 63, Anjananagar, Vishwaneedam post, Bangaluru 560091, Karnataka, India.
  • Manohar TS; Department of Biosciences, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, A.P. 515 134, India.
  • Venketesh S; Department of Biosciences, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, A.P. 515 134, India.
  • Asad M; Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Center of Excellence for Advanced Materials Research (CEAMR), King Abdulaziz University, Jeddah 21589, Saudi Arabia.
  • Asiri AM; Chemistry Department, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Center of Excellence for Advanced Materials Research (CEAMR), King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Bioorg Chem ; 81: 134-143, 2018 12.
Article em En | MEDLINE | ID: mdl-30121001
ABSTRACT
Novel highly functionalized 2-amino-4H-pyrans were achieved in excellent yields under simple grinding at ambient temperature and were assessed for their potential for treating Alzheimer's disease (AD). The 2-amino-4H-pyran bearing nitro groups on both the aryl rings showed the highest activity, with an IC50 of 1.98 ±â€¯0.09 µM against acetylcholinesterase (AChE) and 10.62 ±â€¯0.21 µM against butyrylcholinesterase (BChE), the inhibition mechanisms on AChE and BChE receptors were revealed by means of molecular docking simulations.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Acetilcolinesterase / Piranos / Butirilcolinesterase / Inibidores da Colinesterase Limite: Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Acetilcolinesterase / Piranos / Butirilcolinesterase / Inibidores da Colinesterase Limite: Humans Idioma: En Ano de publicação: 2018 Tipo de documento: Article