| Title : Identification of two arylimides as cholinesterase inhibitors and testing of propranolol addition on impaired rat memory - Cipres-Flores_2020_Drug.Dev.Res_81_256 |
| Author(s) : Cipres-Flores FJ , Farfan-Garcia ED , Andrade-Jorge E , Cuevas-Hernandez RI , Tamay-Cach F , Martinez-Archundia M , Trujillo-Ferrara JG , Soriano-Ursua MA |
| Ref : Drug Dev Res , 81 :256 , 2020 |
| Abstract : Alzheimer's disease (AD) is clearly linked to the decline of acetylcholine (ACh) effects in the brain. These effects are regulated by the hydrolytic action of acetylcholinesterase (AChE). Therefore, a central palliative treatment of AD is the administration of AChE inhibitors although additional mechanisms are currently described and tested for generating advantageous therapeutic strategies. In this work, we tested new arylamides and arylimides as potential inhibitors of AChE using in silico tools. Then, these compounds were tested in vitro, and two selected compounds, C7 and C8, as well as propranolol showed inhibition of AChE. In addition, they demonstrated an advantageous acute toxicity profile compared to that of galantamine as a reference AChE inhibitor. in vivo evaluation of memory performance enhancement was performed in an animal model of cognitive disturbance with each of these compounds and propranolol individually as well as each compound combined with propranolol. Memory improvement was observed in each case, but without a significant additive effect with the combinations. |
| ESTHER : Cipres-Flores_2020_Drug.Dev.Res_81_256 |
| PubMedSearch : Cipres-Flores_2020_Drug.Dev.Res_81_256 |
| PubMedID: 31875337 |
Cipres-Flores FJ, Farfan-Garcia ED, Andrade-Jorge E, Cuevas-Hernandez RI, Tamay-Cach F, Martinez-Archundia M, Trujillo-Ferrara JG, Soriano-Ursua MA (2020)
Identification of two arylimides as cholinesterase inhibitors and testing of propranolol addition on impaired rat memory
Drug Dev Res
81 :256
Cipres-Flores FJ, Farfan-Garcia ED, Andrade-Jorge E, Cuevas-Hernandez RI, Tamay-Cach F, Martinez-Archundia M, Trujillo-Ferrara JG, Soriano-Ursua MA (2020)
Drug Dev Res
81 :256