Insights into structure-activity relationships of 3-arylhydrazonoindolin-2-one derivatives for their multitarget activity on 尾-amyloid aggregation and neurotoxicity was written by Purgatorio, Rosa;de Candia, Modesto;De Palma, Annalisa;De Santis, Francesco;Pisani, Leonardo;Campagna, Francesco;Cellamare, Saverio;Altomare, Cosimo Damiano;Catto, Marco. And the article was included in Molecules in 2018.Computed Properties of C10H9NO2 This article mentions the following:
A series of new 3-(2-arylhydrazono)indolin-2-one derivatives I [R = H, n-Bu, 5-MeO; R1 = H; R2 = H, Br; R3 = H, Me, cyclopropyl, Bn, (CH2)2C6H5, (CH2)3C6H5; R4 = H, Me; RR1 = OCH2O; Ar = 4-iPrC6H4, 4-NCC6H4, 1-naphthyl, etc.]was synthesized and assayed, investigating the effects of substitutions on both the indole core and arylhydrazone moiety. Compared with the reference we disclosed equipotent derivatives bearing alkyl substituents at the indole nitrogen and fairly tolerated bioisosteric replacements at the arylhydrazone moiety. For most of the investigated compounds, the inhibition of A尾40 aggregation (expressed as pIC50) was found to be correlated with lipophilicity, as assessed by a reversed-phase HPLC method, through a bilinear relationship. The compound I [R = MeO, R1 = R2 = H, R3 = cyclopropyl, R4 = H Ar = 4-iPrC6H4] was tested in cell-based assays of A尾42 oligomer toxicity and oxidative stress induced by hydrogen peroxide, showing significant cytoprotective effects. This study confirmed the versatility of isatin in preparing multitarget small mols. affecting different biochem. pathways involved in Alzheimer’s disease. In the experiment, the researchers used many compounds, for example, 5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1Computed Properties of C10H9NO2).
5-Methoxy-1H-indole-3-carbaldehyde (cas: 10601-19-1) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. Moreover, it is known that it controls biofilm formation. However, the role of indole in the cell has not been fully elucidated.Computed Properties of C10H9NO2
Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles