| Title : Exploring indole-based-thiadiazole derivatives as potent acetylcholinesterase and butyrylcholinesterase enzyme inhibitors - Taha_2021_Int.J.Biol.Macromol__ |
| Author(s) : Taha M , Rahim F , Uddin N , Khan IU , Iqbal N , Anouar EH , Salahuddin M , Farooq RK , Gollapalli M , Khan KM , Zafar A |
| Ref : Int J Biol Macromol , : , 2021 |
| Abstract : Indole based thiadiazole derivatives (1-18) were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition. The IC(50) values of the synthesized analogues ranging between 0.17 +/- 0.05 to 33.10 +/- 0.6 microM against (AChE) and 0.30 +/- 0.1 to 37.60 +/- 0.6 microM against (BChE) enzymes. Among the series compounds 8 (IC(50) = 0.17 +/- 0.05 microM) (IC(50) = 0.30 +/- 0.1 microM), 9 (IC(50) = 0.30 +/- 0.05 microM) (IC(50) = 0.60 +/- 0.05 microM) and 10 (IC(50) = 1.30 +/- 0.1 microM) (IC(50) = 2.60 +/- 0.1) were found to be the most potent analogues bearing para, ortho, and meta-fluoro substitutions on phenyl ring attached to thiadiazole. In addition, all the synthesized scaffolds were characterized by using (1)H NMR, (13)C NMR spectroscopy, and high-resolution Mass Spectrometry (HR-MS). To apprehend the binding mode of interaction of the most potent synthesized derivatives, a molecular docking study was performed. |
| ESTHER : Taha_2021_Int.J.Biol.Macromol__ |
| PubMedSearch : Taha_2021_Int.J.Biol.Macromol__ |
| PubMedID: 34390751 |
Taha M, Rahim F, Uddin N, Khan IU, Iqbal N, Anouar EH, Salahuddin M, Farooq RK, Gollapalli M, Khan KM, Zafar A (2021)
Exploring indole-based-thiadiazole derivatives as potent acetylcholinesterase and butyrylcholinesterase enzyme inhibitors
Int J Biol Macromol
:
Taha M, Rahim F, Uddin N, Khan IU, Iqbal N, Anouar EH, Salahuddin M, Farooq RK, Gollapalli M, Khan KM, Zafar A (2021)
Int J Biol Macromol
: