54117-37-2Relevant academic research and scientific papers
Design, synthesis and evaluation of carbazole derivatives as potential antimicrobial agents
Xue, Yi-Jie,Li, Ming-Yue,Jin, Xue-Jun,Zheng, Chang-Ji,Piao, Hu-Ri
, p. 295 - 306 (2021/01/13)
Five series of novel carbazole derivatives containing an aminoguanidine, dihydrotriazine, thiosemicarbazide, semicarbazide or isonicotinic moiety were designed, synthesised and evaluated for their antimicrobial activities. Most of the compounds exhibited potent inhibitory activities towards different bacterial strains (including one multidrug-resistant clinical isolate) and one fungal strain with minimum inhibitory concentrations (MICs) between 0.5 and 16 μg/ml. Compounds 8f and 9d showed the most potent inhibitory activities (MICs of 0.5–2 μg/ml). Furthermore, compounds 8b, 8d, 8f, 8k, 9b and 9e with antimicrobial activities were not cytotoxic to human gastric cancer cell lines (SGC-7901 and AGS) or a normal human liver cell line (L-02). Structure–activity relationship analyses and docking studies implicated the dihydrotriazine group in increasing the antimicrobial potency and reducing the toxicity of the carbazole compounds. In vitro enzyme activity assays suggested that compound 8f binding to dihydrofolate reductase might account for the antimicrobial effect.
Synthesis of carbazole derivatives containing chalcone analogs as non-intercalative topoisomerase II catalytic inhibitors and apoptosis inducers
Li, Peng-Hui,Jiang, Hong,Zhang, Wen-Jin,Li, Yong-Lian,Zhao, Min-Cong,Zhou, Wei,Zhang, Lan-Yue,Tang, Ya-Dong,Dong, Chang-Zhi,Huang, Zhi-Shu,Chen, Hui-Xiong,Du, Zhi-Yun
, p. 498 - 510 (2018/01/17)
Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity. Further mechanism studies revealed that CDCAs function as non-intercalative Topo II catalytic inhibitors. Moreover, some CDCAs showed micromolar cytotoxic activities. The most potent compound 3h exhibited notable growth inhibition against four human cancer cell lines. Flow cytometric analysis revealed that compounds 3d and 3h arrested the HL-60 cells in sub G1 phase by induction of apoptosis. It was further confirmed by Annexin-V-FITC binding assay. Western blot analysis revealed that compound 3h induces apoptosis likely through the activation of caspase proteins.
Synthesis and biological evaluation of novel carbazole-rhodanine conjugates as topoisomerase II inhibitors
Jiang, Hong,Zhang, Wen-Jin,Li, Peng-Hui,Wang, Jian,Dong, Chang-Zhi,Zhang, Kun,Chen, Hui-Xiong,Du, Zhi-Yun
supporting information, p. 1320 - 1323 (2018/03/21)
In this study, a series of carbazole-rhodanine conjugates was synthesized and evaluated for their Topoisomerase II inhibition potency as well as cytotoxicity against a panel of four human cancer cell lines. Among these thirteen compounds, 3a, 3b, 3g, and
Azahelicenes as visible light photoinitiators for cationic and radical polymerization: Preparation of photoluminescent polymers and use in high performance LED projector 3D printing resins
Al Mousawi, Assi,Dumur, Frédéric,Garra, Patxi,Toufaily, Joumana,Hamieh, Tayssir,Goubard, Fabrice,Bui, Thanh-Tuan,Graff, Bernadette,Gigmes, Didier,Pierre Fouassier, Jean,Lalevée, Jacques
, p. 1189 - 1199 (2017/03/05)
In this article, novel azahelicenes (AZs) were synthesized and proposed as high performance visible light photoinitiators for both the free radical polymerization of acrylates and the cationic polymerization (CP) of epoxides upon visible light exposure us
Novel carbazole skeleton-based photoinitiators for led polymerization and LED projector 3D printing
Mousawi, Assi Al,Garra, Patxi,Dumur, Frédéric,Bui, Thanh-Tuan,Goubard, Fabrice,Toufaily, Joumana,Hamieh, Tayssir,Graff, Bernadette,Gigmes, Didier,Fouassier, Jean Pierre,Lalevée, Jacques
supporting information, (2018/01/12)
Radical chemistry is a very convenient way to produce polymer materials. Here an application of a particular photoinduced radical chemistry is illustrated. Seven new carbazole derivatives Cd1–Cd7 are incorporated and proposed as high performance near-UV photoinitiators for both the free radical polymerization (FRP) of (meth)acrylates and the cationic polymerization (CP) of epoxides utilizing Light Emitting Diodes LEDs @405 nm. Excellent polymerization-initiating abilities are found and high final reactive function conversions are obtained. Interestingly, these new derivatives display much better near-UV polymerization-initiating abilities compared to a reference UV absorbing carbazole (CARET 9H-carbazole-9-ethanol) demonstrating that the new substituents have good ability to red shift the absorption of the proposed photoinitiators. All the more strikingly, in combination with iodonium salt, Cd1–Cd7 are likewise preferred as cationic photoinitiators over the notable photoinitiator bis(2,4,6-trimethylbenzoyl)phenylphosphine oxide (BAPO) for mild irradiation conditions featuring their remarkable reactivity. In particular their utilization in the preparation of new cationic resins for LED projector 3D printing is envisioned. A full picture of the included photochemical mechanisms is given.
Substituted Carbazoles-A New Class of Anthelmintic Agent
Rennison, David,Gueret, Stephanie M.,Laita, Olivia,Bland, Ross J.,Sutherland, Ian A.,Boddy, Ian K.,Brimble, Margaret A.
, p. 1268 - 1276 (2016/11/25)
A series of novel carbazoles were synthesized based on structural modifications to lead carbazole 1 (EC100≤2.5M against Haemonchus contortus in vitro), which was revealed in a small molecule screening program as a potentially promising platform for the development of new anthelmintic drugs. Subsequently, analogues 19, 21, 41, 42 (EC100≤ 1.25M, all), and 39 (EC100≤0.625M) were demonstrated to exhibit enhanced in vitro anthelmintic activity over the lead structure, with compound 39 also being shown to be active in vivo against Heligmosomoides polygyrus.
Compound containing benzoxazole and carbazole constitutional units and application thereof
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Paragraph 0012, (2016/10/07)
The invention discloses a compound 1,1-di(benzoxazole-2-yl)-2-(N-benzyl carbazole-2-yl) ethylene containing benzoxazole and carbazole constitutional units and the application thereof. The molecular structural formula of the compound 1,1-di(benzoxazole-2-y
Carbazole inhibitors of histamine receptors for the treatment of disease
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Page/Page column 41, (2012/01/04)
The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
CARBAZOLE COMPOUND
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Page/Page column 82, (2010/11/28)
The present invention provides a carbazole compound represented by formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R1 is a hydrogen atom, etc; R2 is a lower alkoxy group, etc; and R3 is a hydrogen atom, etc. The carbazole compound or salt thereof of the present invention induces the production of TFF, and thus is usable for the treatment and/or prevention of disorders such as alimentary tract diseases, oral diseases, upper respiratory tract diseases, respiratory tract diseases, eye diseases, cancers, and wounds.
New carbazole alkaloids from Murraya euchrestifolia
Ito,Okahana,Wu,Wang,Lai,Kuoh,Furukawa
, p. 230 - 232 (2007/10/02)
Two new monomeric and one dimeric carbazole alkaloids were isolated from root bark of Murraya euchrestifolia HAYATA collected in Taiwan. Their structures were elucidated by spectrometric and synthetic studies. The structures of the monomeric carbazoles were assigned as 3-formyl-7-hydroxy-9H-carbazole (1) and N-methoxy-3-hydroxymethyl 9H-carbazole (2). The dimeric carbazole, named chrestifoline-D (9), was found to be identical with the oxidation product of bismurrayafoline-A (10).
