Isatin-tethered halogen-containing acylhydrazone derivatives as monoamine oxidase inhibitor with neuroprotective effect.

ABSTRACT: Sixteen isatin-based hydrazone derivatives (IS1-IS16) were synthesized and assessed for their ability to inhibit monoamine oxidases (MAOs). All the molecules showed improved inhibitory MAO-B activity compared to MAO-A. Compound IS7 most potently inhibited MAO-B with an IC₅₀ value of 0.082 μM, followed by IS13 and IS6 (IC₅₀ = 0.104 and 0.124 μM, respectively). Compound IS15 most potently inhibited MAO-A with an IC₅₀ value of 1.852 μM, followed by IS3 (IC₅₀ = 2.385 μM). Compound IS6 had the highest selectivity index (SI) value of 263.80, followed by IS7 and IS13 (233.85 and 212.57, respectively). In the kinetic study, the K_i values of IS6, IS7, and IS13 for MAO-B were 0.068 ± 0.022, 0.044 ± 0.002, and 0.061 ± 0.001 μM, respectively, and

SUBMITTER: Kumar S 

PROVIDER: S-EPMC10787790 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature