15096-16-9Relevant academic research and scientific papers
Indium(iii)-catalyzed efficient synthesis of 3-arylhydrazonoindolin-2-ones and their fluorescent metal sensing studies
Devkota, Shreedhar,Lee, Yong Rok,Mohandoss, Sonaimuthu
supporting information, p. 3640 - 3644 (2022/03/07)
An efficient and facile In(iii)-catalyzed reaction of 3-diazoindolin-2-ones with different arylhydrazines is demonstrated. This approach offers a rapid synthetic route to diversely functionalized 3-arylhydrazonoindolin-2-ones in good yields. This novel protocol introduces biologically and photo-functionally interesting hydrazones at the 3-position of indolin-2-ones. The synthesized compounds are further used to investigate their fluorescence responses toward heavy metal ions. This journal is
Pharmacophore modeling and 3D-QSAR study of indole and isatin derivatives as antiamyloidogenic agents targeting Alzheimer’s disease
Purgatorio, Rosa,Gambacorta, Nicola,Catto, Marco,de Candia, Modesto,Pisani, Leonardo,Espargaró, Alba,Sabaté, Raimon,Cellamare, Saverio,Nicolotti, Orazio,Altomare, Cosimo D.
, (2021/01/12)
Thirty-six novel indole-containing compounds, mainly 3-(2-phenylhydrazono) isatins and structurally related 1H-indole-3-carbaldehyde derivatives, were synthesized and assayed as inhibitors of beta amyloid (Aβ) aggregation, a hallmark of pathophysiology of Alzheimer’s disease. The newly synthesized molecules spanned their IC50 values from sub- to two-digit micromolar range, bearing further information into structure-activity relationships. Some of the new compounds showed interesting multitarget activity, by inhibiting monoamine oxidases A and B. A cell-based assay in tau overexpressing bacterial cells disclosed a promising additional activity of some derivatives against tau aggregation. The accumulated data of either about ninety published and thirty-six newly synthesized molecules were used to generate a pharmacophore hypothesis of antiamyloidogenic activity exerted in a wide range of potencies, satisfactorily discriminating the ‘active’ compounds from the ‘inactive’ (poorly active) ones. An atom-based 3D-QSAR model was also derived for about 80% of ‘active’ compounds, i.e., those achieving finite IC50 values lower than 100 μM. The 3D-QSAR model (encompassing 4 PLS factors), featuring acceptable predictive statistics either in the training set (n = 45, q2 = 0.596) and in the external test set (n = 14, r2ext = 0.695), usefully complemented the pharmacophore model by identifying the physicochemical features mainly correlated with the Aβ anti-aggregating potency of the indole and isatin derivatives studied herein.
3-DIARYL- AND 3-DIALKYLGLYCOLOYLHYDRAZONES OF SUBSTITUTED ISATINS
Maslivets, A. N.,Berdinskii, I. S.
, p. 755 - 759 (2007/10/02)
The 3-diarylglycoloylhydrazones of substituted isatins were obtained by the condensation of diarylglycolohydrazides and the corresponding isatins. 3-Dialkylglycoloylhydrazones of substituted isatins were obtained by transhydrazonation of α-propylbenzylide
A Study of the Structure of Hydrazones of Indole-2,3-dione and 1-Methylindole-2,3-dione with Nuclear Magnetic Resonance Spectroscopy
Snavely, Fred A.,Un, Sun
, p. 2764 - 2766 (2007/10/02)
Nuclear magnetic resonance was used to determine the structure of mono- and disubstituted hydrazones of indole-2,3-dione and 1-methylindole-2,3-dione.The assignment of the hydrazone form to all of the monosubstituted derivatives is supported by infrared d
