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Paper(s) concerning 4-aminopyridine-1,3,4-oxadiazole-9

1 reference(s) found.
Listing paper details in reverse chronological order.
We are grateful to Keith Bradnam for improvment of this script

Title: Design and development of 1,3,4-oxadiazole derivatives as potential inhibitors of acetylcholinesterase to ameliorate scopolamine-induced cognitive dysfunctions
Mishra P, Sharma P, Tripathi PN, Gupta SK, Srivastava P, Seth A, Tripathi A, Krishnamurthy S, Shrivastava SK
Ref: Bioorg Chem, 89:103025, 2019 : PubMed
Abstract


ESTHER: Mishra_2019_Bioorg.Chem_89_103025
PubMedSearch: Mishra 2019 Bioorg.Chem 89 103025
PubMedID: 31176239
Inhibitor(s) related to this paper: 4-aminopyridine-1,3,4-oxadiazole-9

Abstract

The novel hybrids bearing 4-aminopyridine (4-AP) tethered with substituted 1,3,4-oxadiazole nucleus were designed, synthesized, and evaluated for their potential AChE inhibitory property along with significant antioxidant potential. The inhibitory potential (IC50) of synthesized analogs was evaluated against human cholinesterases (hAChE and hBChE) using Ellman's method. Among all the compounds, 9 with 4-hydroxyl substituent showed maximum hAChE inhibition with the non-competitive type of enzyme inhibition (IC50=1.098microM; Ki=0.960microM). Further, parallel artificial membrane permeation assay (PAMPA-BBB) showed significant BBB permeability in most of the synthesized compounds. Meanwhile, compound 9 also inhibited AChE-induced Abeta aggregation (38.2-65.9%) by thioflavin T assay. The in vivo behavioral studies showed dose-dependent improvement in learning and memory by compound 9. The ex vivo studies also affirmed the significant AChE inhibition and antioxidant potential of compound 9 in brain homogenates.