1313405-84-3Relevant articles and documents
Cholinesterases inhibition and molecular modeling studies of piperidyl-thienyl and 2-pyrazoline derivatives of chalcones
Shah, Muhammad Shakil,Khan, Shafi Ullah,Ejaz, Syeda Abida,Afridi, Saifullah,Rizvi, Syed Umar Farooq,Najam-ul-Haq, Muhammad,Iqbal, Jamshed
, p. 615 - 624 (2017/01/16)
Super-activation of cholinesterases (acetylcholinesterase and butyrylcholinesterase) are linked to various neurological problems most precisely Alzheimer's disease (AD), which leads to senile dementia. Therefore, cholinesterases (AChE & BChE) inhibition are considered as a promising strategy for the treatment of Alzheimer's disease. FDA approved drugs for the treatment of AD, belong to a group of cholinesterase inhibitors. However, none of them is able to combat or completely abrogate the disease progression. Herein, we report a series of newly synthesized chalcone derivatives with anti-AD potential. For this purpose, a series of piperidyl-thienyl and 2-pyrazoline derivatives of chalcones were tested for their cholinesterases (AChE & BChE) inhibitory activity. All compounds were found as selective inhibitor of AChE. In piperidyl chalcones derivatives compound 1e having IC50 of 0.16?±?0.008?μM and 2m in 2-pyrazoline chalcones with IC50 of 0.13?±?0.006?μM, were found to be the most potent inhibitors of AChE, exhibiting ≈142 and?≈?173-fold greater inhibitory potential compared to the reference inhibitor i.e., Neostigmine (IC50?±?SEM?=?22.2?±?3.2?μM). Molecular docking studies of most potent inhibitors were carried out to investigate the binding interactions inside the active site. Molecular docking study revealed that potent compounds and co-crystalized ligand had same binding orientation within the active site of target enzyme. Most of these compounds are selective inhibitors of AChE with a potential use against progressive neurodegenerative disorder and age related problems.
Novel quinolyl-thienyl chalcones and their 2-pyrazoline derivatives with diverse substitution pattern as antileishmanial agents against Leishmania major
Rizvi, Syed Umar Farooq,Siddiqui, Hamid Latif,Ahmad, Muhammad Nisar,Ahmad, Matloob,Bukhari, Mujahid Hussain
, p. 1322 - 1333 (2012/07/30)
A series of twenty-two new pyrazoline derivatives was prepared from quinoline-based chalcones which in turn were synthesized by condensing formylquinolines with diverse acetylthiophenes. The titled compounds were characterized by spectroscopic techniques (NMR, IR and MS) and elemental analysis. All the compounds were screened for antileishmanial activities. Compounds 1e, 1f, 2a, 2c, 2d, 2g, 2k, and 4a were found potentially active antileishmanial agents. Bioassay results show that the type and positions of the substituents seem to be critical for their antileishmanial activities. Springer Science+Business Media, LLC 2011.
