29236-09-7

Upstream product

• 1122-17-4 dichloromaleic acid anhydride 
• 106-47-8 4-chloro-aniline 
• 108-31-6 maleic anhydride 
• 7242-16-2 N-4-chlorophenyl-maleamic acid 
• 1631-29-4 N-(4-chlorophenyl)maleimide 
• 6943-00-6 1-(4-chlorophenyl)pyrrolidine-2,5-dione 

Downstream Products

• 886055-36-3 3,4-bis(4-ethoxycarbonyl-3-hydroxy-5-methyl-2-thienyl)-1-(4-chlorophenyl)-1H-pyrrol-2,5-dione 
• 1109273-49-5 2-(4-chlorophenyl)-pyrrolo[3,4-b][1,4]benzoxazine-1,3(2H,9H)-dione 
• 1109273-73-5 2-(4-chlorophenyl)-7-tert-butyl-pyrrolo[3,4-b][1,4]benzoxazine-1,3(2H,9H)-dione 
• 1109273-62-2 2-(4-chlorophenyl)-7-chloro-pyrrolo[3,4-b][1,4]benzoxazine-1,3(2H,9H)-dione 
• 1449434-80-3 C₁₈H₁₀Cl₂N₂O₂ 
• 143947-24-4 6-(4-Chloro-phenyl)-2-thioxo-[1,3]dithiolo[5,6][1,4]dithiino[2,3-c]pyrrole-5,7-dione 

Relevant academic research and scientific papers

Application of maleimide compound as chitin synthase inhibitor

The invention discloses an application of a maleimide compound as shown in a formula I. In the formula I, R0 is phenyl, benzyl, phenethyl, phenylpropyl, p-fluorophenyl, p-chlorophenyl, p-bromophenyl,p-methoxyphenyl, p-methylphenyl or p-hydroxyphenyl, R1 is hydrogen, methyl, phenyl or chlorine; and R2 is hydrogen, methyl, phenyl or chlorine. The provided maleimide compound has a good inhibition effect on chitin synthase.

Anti-leishmanial and cytotoxic activities of a series of maleimides: Synthesis, biological evaluation and structure-activity relationship

In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 50 50 > 10 μg/mL). The anti-leishmanial activities of 16 and 42 were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development.

Synthesis and biological evaluation of 3-chloro-4-(indol-3-yl)-2,5- pyrroledione derivatives as antitumor agents

A series of 3-chloro-4-(indol-3-yl)-2,5-pyrroledione derivatives were synthesized and evaluated for their cytotoxic activities in vitro against five human cancer cell lines (K562, A549, ECA-109, KB and SMMC-7721). Most compounds displayed potent cytotoxicity with IC50 values in low micromolar range. The results showed that the existence of the chlorine atom at 3-position on the pyrroledione ring was crucial for the activity. Compound 6a, the most potent one (IC50: 0.67～3.93 μM), would be a promising template for further development of novel antitumor agents.

Synthesis of novel 1,4-benzoxazine-2,3-dicarboximides from maleic anhydride and substituted aromatic amines

A series of novel 1,4-benzoxazine-2,3-dicarboximides starting from maleic anhydride and substituted aromatic amines were synthesized. Copyright Taylor & Francis Group, LLC.

Synthesis and characterization of new compounds containing 1,4-dithiintetracarboxydiimide units

New compounds containing 1,4-dithiintetracarboxydiimide units were synthesized by the disubstitution reaction of N-substituted 2,3- dichloromaleimide with sodium sulflde nonahydrate or thiourea. IR, UV-vis and 1H-NMR spectroscopy, as well as elemental analysis, confirmed their structures. Thermal conversion of 1,4-dithiine ring to thiophene was monitored by differential calorimetry (DSC) and thermogravimetric (TGA) measurements.

In vitro antifungal properties, structure-activity relationships and studies on the mode of action of N-phenyl, N-aryl, N-phenylalkyl maleimides and related compounds

The synthesis, in vitro antifungal evaluation and structure-activity relationship studies of 14 compounds of the N-phenyl-, N-aryl-, N-phenylalkyl- maleimide and 3,4-dichloromaleimide series are reported. The compounds were evaluated against a panel of standardized yeasts and filamentous fungi as well as clinical isolates of Candida albicans. The activities of N-phenylalkyl-3,4- dichloromaleimide derivatives but not those of N-phenylalkyl-maleimide derivatives showed to be dependent on the length of the alkyl chain. N-Phenylpropyl-3,4-dichloromaleimide showed the broadest spectrum of action and lower minimal inhibitory concentrations (MIC) in all of the fungi tested. The nitrogen-carbon distance between the two rings seems to play an important role in the antifungal behavior of these compounds. The most active structure showed inhibited (1,3)β-D-glucan and chitin synthases, enzymes that catalyze the synthesis of the major fungal cell-wall polymers. ECV · Editio Cantor Verlag, Aulendorf (Germany).