| Title : Synthesis, molecular modeling and cholinesterase inhibitory effects of 2-indolinone-based hydrazinecarbothioamides - Demir-Yazici_2021_Future.Med.Chem__ |
| Author(s) : Demir-Yazici K , Apaydin C B , Soylu-Eter O , Ozsoy N , Karali N |
| Ref : Future Med Chem , : , 2021 |
| Abstract : Background: 2-Indolinone-based hydrazinecarbothioamides carrying a 3-phenylsulfonamide moiety (7-9) were designed by replacement of donepezil's pharmacophore group indanone with a 2-indolinone ring. Method: Compounds 7-9 were synthesized by reaction of N-(3-sulfamoylphenyl)hydrazinecarbothioamide (6) with 1H-indolin-2,3-diones (1-3). Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory effects of compounds 7-9 were assayed. Molecular modeling studies of 5-chloro-1,7-dimethyl-substituted compound 8e were carried out to determine the possible binding interactions at the active site of AChE. Results: Compound 8e showed the strongest inhibition against AChE (K(i) = 0.52 +/- 0.11 microM) as well as the highest selectivity (SI = 37.69). The selectivity for AChE over BuChE of compound 8e was approximately 17-times higher than donepezil and 26-times higher than galantamine. Conclusion: Further development of compounds 7-9 may present new promising agents for Alzheimer's treatment. |
| ESTHER : Demir-Yazici_2021_Future.Med.Chem__ |
| PubMedSearch : Demir-Yazici_2021_Future.Med.Chem__ |
| PubMedID: 34755546 |
Demir-Yazici K, Apaydin C B, Soylu-Eter O, Ozsoy N, Karali N (2021)
Synthesis, molecular modeling and cholinesterase inhibitory effects of 2-indolinone-based hydrazinecarbothioamides
Future Med Chem
:
Demir-Yazici K, Apaydin C B, Soylu-Eter O, Ozsoy N, Karali N (2021)
Future Med Chem
: