29775-73-3

Upstream product

• 91-56-5 indole-2,3-dione 
• 104-94-9 4-methoxy-aniline 
• 42366-35-8 hydroxyimino-N-phenylacetamide 
• 62-53-3 aniline 

Downstream Products

• 2400-97-7 3-(4-methoxyphenyl)-1H,3H-quinazolin-2,4-dione 
• 57644-26-5 3-(4-meth-oxyphenylimino)-1-(piperidin-1-ylmethyl)indolin-2-one 
• 57644-26-5 3-[(Z)-4-Methoxy-phenylimino]-1-piperidin-1-ylmethyl-1,3-dihydro-indol-2-one 
• 29775-74-4 1-Morpholinomethyl-3-(4-methoxyphenyl)imino-1H-indole-2,3-dione 
• 29775-74-4 3-(4-methoxy-phenylimino)-1-morpholin-4-ylmethyl-1,3-dihydro-indol-2-one 
• 111259-65-5 C₁₉H₁₆N₂O₅S 
• 116222-17-4 3-(4-Methyl-benzoylamino)-2-oxo-1,2-dihydro-quinoline-4-carboxylic acid (4-methoxy-phenyl)-amide 
• 79560-74-0 NSC₇₃₃₀₆ 
• 59618-77-8 3'-(4-methoxyphenyl)-spiro[3H-indole-3,2'-thiazolidine] 2,4'-(1H)-dione 
• 91870-66-5 3'-[4-methoxyphenyl]-5'-methyl-spiro[3H-indole-3,2'-thiazolidine]-2,4'(1H)-dione 
• 97692-97-2 C₂₃H₂₅N₃O₃S 
• 97692-88-1 1-Benzyl-3'-(4-methoxyphenyl)spiro<3H-indole-3,2'-tetrahydro-1,3-thiazine>-2,4'(1H)-dione 
• 97692-96-1 C₂₄H₂₇N₃O₃S 
• 97692-95-0 1-Morpholinomethyl-3'-(4-methoxyphenyl)spiro<3H-indole-3,2'-tetrahydro-1,3-thiazine>-2,4'(1H)-dione 

Relevant academic research and scientific papers

Theoretical molecular properties prediction, docking and antimicrobial studies on Anisidine-Isatin Schiff bases

The continuous intake of a specific antibiotic for diseases is continuously reducing the immunity of the human in course of time, which includes Covid-19 treatment. Recent research on Schiff bases shows the promising biological activities and good antibac

Synthesis of 1,3-diaryl-spiro[azetidine-2,3′-indoline]-2′,4-diones: Via the Staudinger reaction: Cis - Or trans -diastereoselectivity with different addition modes

A new synthetic approach for realizing biologically relevant bis-aryl spiro[azetidine-2,3′-indoline]-2′,4-diones was developed based on Staudinger ketene-imine cycloaddition through the one-pot reaction of substituted acetic acids and Schiff bases in the presence of oxalyl chloride and an organic base. A series of [azetidine-2,3′-indoline]-2′,4-diones were synthesized using this method. For comparison, the same compounds were obtained using a known technique, where ketene is generated from pre-synthesized acyl chloride. It was shown that the use of oxalyl chloride for ketene generation in the one-pot reaction at room temperature allows for the reversal of the diastereoselectivity of spiro-lactam formation, unlike previously described procedures.

Design, synthesis and biological activity of novel tacrine-isatin Schiff base hybrid derivatives

A series of novel tacrine-isatin Schiff base hybrid derivatives (7a-p)were designed, synthesized and evaluated as multi-target candidates against Alzheimer's disease (AD). The biological assays indicated that most of these compounds displayed potent inhibitory activity toward acetylcholinesterase (AChE)and butyrylcholinesterase (BuChE)and specific selectivity for AChE over BuChE. It was also found that they act as excellent metal chelators. The compounds 7k and 7m were found to be good inhibitors of AChE-induced amyloid-beta (Aβ)aggregation. Most of the compounds inhibited AChE with the IC50 values, ranging from 0.42 nM to 79.66 nM. Amongst them, 7k, 7m and 7p, all with a 6 carbon linker between tacrine and isatin Schiff base exhibited the strongest inhibitory activity against AChE with IC50 values of 0.42 nM, 0.62 nM and 0.95 nM, respectively. They were 92-, 62- and 41-fold more active than tacrine (IC50 = 38.72 nM)toward AChE. Most of the compounds also showed a potent BuChE inhibition among which 7d with an IC50 value of 0.11 nM for BuChE is the most potent one (56-fold more potent than that of tacrine (IC50 = 6.21 nM)). In addition, most compounds exhibited the highest metal chelating property. Kinetic and molecular modeling studies revealed that 7k is a mixed-type inhibitor, capable of binding to catalytic and peripheral site of AChE. Our findings make this hybrid scaffold an excellent candidate to modify current drugs in treating Alzheimer's disease (AD).

Stereocontrolled [3+2] Cycloaddition of Donor-Acceptor Cyclopropanes to Iminooxindoles: Access to Spiro[oxindole-3,2′-pyrrolidines]

A novel stereocontrolled assembly of spiro[oxindole-3,2′-pyrrolidines] via [3+2]-cycloaddition of donor-acceptor cyclopropanes to electron-poor ketimines, iminooxindoles, was developed. The method allows for efficient employment of common readily available donor-acceptor cyclopropanes, functionalized with ester, keto, nitro, cyano etc. groups, and N-unprotected iminooxindoles. The stereospecificity of the initial SN2-like imine attack on a cyclopropane molecule together with a high diastereoselectivity of further C-C bond formation facilitate a rapid access to spiro[oxindole-3,2′-pyrrolidines] in their optically active forms. Preliminary in vitro testing of the synthesized compounds against LNCaP (p53+) and PC-3 (p53-) cells revealed good antiproliferative activities and p53-selectivity indices for several compounds that are intriguing in terms of their further investigation as inhibitors of MDM2-p53 interaction.

Microwave-assisted synthesis and evaluation of indole derivatives as potential anthelmintic agents

An efficient method is developed and exploited for the synthesis of indole derivatives via microwave-assisted technology. By considering the advantage microwave synthesis in terms of high efficient energy, indole derivatives are prepared. In the current study, the Schiff's bases are first synthesized by reaction of 1H-indole-2,3-dione (isatin) with various substituted anilines in presence of acetic acid under microwave irradiation. Then the Mannich bases are produced by condensation of Schiff bases with different secondary amines in the presence of formaldehyde. The newly synthesized compounds are characterized by TLC report and spectral data followed by evaluation for anthelmintic activity against Pheretima posthuma. Albendazole is used as standard drug for comparative study. The titled compounds are screened for anthelmintic activity at the concentration of 10, 20 and 50 mg/ml. The anthelmintic effect of standard drug Albendazole is also evaluated at 10 mg/ml. The results of present study indicate that some of the tested compounds exhibit significant anthelmintic activity in dose dependent manner.

Leucine rich repeat kinase 2 (LRRK2) inhibitors based on indolinone scaffold: Potential pro-neurogenic agents

Leucine-rich repeat kinase 2 (LRRK2) is one of the most pursued targets for Parkinson's disease (PD) therapy. Moreover, it has recently described its role in regulating Wnt signaling and thus, it may be involved in adult neurogenesis. This new hypothesis

Practical Synthesis, Antidepressant, and Anticonvulsant Activity of 3-Phenyliminoindolin-2-one Derivatives

Herein, a series of 3-phenyliminoindolin-2-one derivatives were designed, synthesized, and screened for their antidepressant and anticonvulsant activities. The IR spectra of the compounds afforded NH stretching (3340-3346 cm-1) bands and C=O stretching (1731-1746 cm-1). In the 1H-NMR spectra of the compounds, N-H protons of indoline ring were observed at 10.65-10.89 ppm generally as broad bands, and 13C-NMR spectra of the compounds C=O were seen at 161.72-169.27 ppm. Interestingly, compounds 3o, 3p and 3r significantly shortened immobility time in the The forced swimming test (FST) and The tail suspension test (TST) at 50 mg/kg dose levels. In addition, compound 3r exhibited higher levels of efficacy than the reference standard fluoxetine but had no effect on locomotor activity in the open-field test. Compound 3r significantly increased serotonin and norepinephrine and the metabolite 5-hydroxyindoleacetic acid in mouse brain, suggesting that the effects of compound 3r may be mediated through these neurotransmitters. In the seizure screen, 15 compounds showed some degree against PTZ-induced seizure at a dose of 100 mg/kg, and the tested compounds did not show any neurotoxicity at a dose of 300 mg/kg in the rotarod test.

Imidazolylpyridine-In(OTf)3 catalyzed enantioselective allylation of ketimines derived from isatins

An enantioselective In(OTf)3-catalyzed allylation of ketimines derived from isatins in the presence of an imidazolylpyridine ligand is described. The reaction proceeded smoothly under mild conditions and resulted in 3-allyl 3-aminooxindoles with good yields and moderate to excellent enantioselectivities (up to 97% ee).

Tin powder-promoted one-pot synthesis of 3-spiro-fused or 3,3′-disubstituted 2-oxindoles

A convenient and efficient method for the constructions of 3-spirooxindole derivatives or 3,3′-disubstituted oxindoles has been developed from one-pot reactions of isatins, hydrazides or aromatic amines, 2-(bromomethyl)acrylic ester and tin powder in the

Synthesis, cytoprotective and anti-Tumor activities of Isatin Schiff bases

A series of simple isatin Schiff bases were synthesized through the condensation reaction. These isatin Schiff bases were characterized by NMR and MS, and the structure was discussed. Then, the cytoprotective and anti-Tumor activities of these compounds were evaluated. The results show that several compounds show protection activity on the apoptosis of PC12 cells induced by H2O2, which are more effective than that of (±) α-Tocophreol (VE) and isatin. Besides, some compounds also show more potent anti-Tumor activity against A549 and P388 cell lines than that of isatin.