3116-49-2Relevant academic research and scientific papers
Application of maleimide compound as chitin synthase inhibitor
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Paragraph 0024-0027; 0096-0099, (2020/07/12)
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
Fan, Yongxian,Lu, Yuele,Chen, Xiaolong,Tekwani, Babu,Li, Xing-Cong,Shen, Yinchu
, (2018/11/24)
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.
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
Lopez, Silvia N.,Castelli, Maria V.,De Campos, Fatima,Correa, Rogerio,Cechinel Filho, Valdir,Yunes, Rosendo A.,Zamora, Miguel A.,Enriz, Ricardo D.,Ribas, Juan C.,Furlan, Ricardo L. E.,Zacchino, Susana A.
, p. 123 - 132 (2007/10/03)
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).
Fungicidal N-substituted maleic acid imides
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, (2008/06/13)
Fungicidally active substituted maleic acid amides of the formula STR1 in which X is hydrogen, chlorine or bromine, X1 is chlorine or bromine, R is alkyl, optionally substituted aryl or optionally substituted aralkyl, R1 to R5/
