21591-87-7

Upstream product

• 91-56-5 indole-2,3-dione 
• 122-01-0 4-chloro-benzoyl chloride 

Downstream Products

• 93065-28-2 4-Chloro-N-[2-(7-methyl-3-oxo-3,4-dihydro-quinoxalin-2-yl)-phenyl]-benzamide 
• 1039045-16-3 10-(4-chlorophenyl)-7,8-benzoquinoline 
• 18600-52-7 2-(4-chlorophenyl)-4H-benzo[d][1,3]oxazin-4-one 
• 1445993-10-1 (2′S,4′R)-ethyl 1-(4-chlorobenzoyl)-2-oxospiro[indoline-3,2′-thiazolidine]-4′-carboxylate 
• 128649-59-2 [5-(4-Chloro-benzoyl)-5H-[1,2,4]triazino[5,6-b]indol-3-yl]-acetonitrile 
• 128649-61-6 (3-Amino-[1,2,4]triazino[5,6-b]indol-5-yl)-(4-chloro-phenyl)-methanone 

Relevant academic research and scientific papers

Studies on potential antiviral compounds. XXIV. New 1-substituted isatin β-thiosemicarbazones

Some new 1-substituted isatin β-thiosemicarbazones were examined for their ability to inhibit the growth of the wild-type strain of vaccinia virus and the isatin β-thiosemicarbazone (IBT) resistant mutant of this virus. Also investigated was the capabilit

Synthesis of some N-aroyl-2-oxindole benzenesulfonamide conjugates with carbonic anhydrase inhibitory activity

Implication of carbonic anhydrases (CAs) in many physiological functions made them attractive therapeutic targets. Herein, we report the synthesis of three series of benzenesulfonamide-based compounds (5a-e, 9a-e and 10a-e) as potential ligands to four of

Selective C?N Bond Cleavage of N-Acylisatins: Towards High Performance Acylation/Arylation/Transamination Reagents

New multipurpose arylation/acylation/transamination reagents, N-acylisatins, have been developed by selective ‘inside-outside’ C?N bond cleavage under different catalytic conditions. As activated amides, N-acylisatins undergo Rh-catalyzed C?H arylation and Pd-catalyzed acylation by cleavage outside the C?N bond, and the desired biaryls and diaryl ketones were obtained in good to excellent yields. Generally, the combination of N-acylisatins with amines leads to a ring-opening reaction and formation of transamination products in a predictable manner through inside C?N bond cleavage. Interestingly, treatment of N-acylisatins with amines lead to unexpected outer-ring transamination products when CsF is added, which shows that CsF can favor the outside C?N bond cleavage path. Notably, this work presents a new strategy for multiple chemical transformations of a single amide to achieve various products by selective C?N bond cleavage. (Figure presented.).

Silver-Mediated Synthesis of 4H-Benzoxazin-4-ones by Intramolecular Decarboxylative O-Acylation Reactions with α-Oxocarboxylic Acid

The first example of an intramolecular decarboxylative acylation reaction for the synthesis of 4H-benzoxazin-4-one derivatives has been described. The silver-mediated reaction has a broad substrate scope and provides a mild and rapid approach to the corre

Synthesis, in vitro, and in cell studies of a new series of [Indoline-3,2′-thiazolidine]-based p53 modulators

Analogues of the previously described spiro[imidazo[1,5-c]thiazole-3, 3′-indoline]-2′,5,7(6H,7aH)-trione p53 modulators were prepared to explore new structural requirements at the thiazolidine domain for the antiproliferative activity and p53 modulation. In cell, antiproliferative activity was evaluated against two human tumor cell lines. Derivative 5-bromo-3′-(cyclohexane carbonyl)-1-methyl-2-oxospiro[indoline-3,2′- thiazolidine] (4n) emerged as the most potent compound of this series, inhibiting in vitro 30% of p53-MDM2 interaction at 5 μM and the cell growth of different human tumor cells at nanomolar concentrations. Docking studies confirmed the interactions of 4n with the well-known Trp23 and Phe19 clefts, explaining the reasons for its binding affinity for MDM2. 4n at 50 nM is capable of inducing the accumulation of p53 protein, inducing significant apoptotic cell death without affecting the cell cycle progression. Comparative studies using nutlin in the same cellular system confirm the potential of 4n as a tool for increasing understanding of the process involved in the nontranscriptional proapoptotic activities of p53.

N-aroylated isatins: Antiglycation activity

A series of N-aroylated isatins 1-15 was synthesized and evaluated for their antiglycation activity. All compounds showed a varying degree of glycation inhibitory activity with IC50 values between 18.01 ± 0.05-693.7 ± 3.0 μM, when compared with the standard (aminoguanidine) having an IC50 = 268.7 ± 12.4 μM. Compound 1 was found to be the most active member of this series with an IC50 = 18.01 ± 0.05 μM. Compound 10 showed an IC50 = 72.5 ± 0.09 μM, whereas compound 7 has an IC50 = 80.18 ± 0.07 μM. Compounds 3, 9, and 13 showed IC50 values 170.2 ± 0.62, 117.91 ± 2.9, 171.3 ± 0.79 μM, respectively. Rest of the compounds along with parent isatin were found to be inactive. The structures of all the synthetic compounds were deduced by spectroscopic analysis.

OXINDOLE COMPOUNDS AND THEIR USES AS THERAPEUTIC AGENTS

This invention is directed to oxindole compounds that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.