52131-82-5Relevant articles and documents
Carbazole isopropanol diamine compound containing 1, 2, 3-triazole as well as preparation method and application of carbazole isopropanol diamine compound
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Paragraph 0047; 0048, (2021/04/03)
The invention relates to a carbazole isopropanol diamine compound containing 1, 2, 3-triazole as well as a preparation method and application of the carbazole isopropanol diamine compound. The compound has a structure as shown in a general formula (I) which is described in the specification. Carbazole is used as a basis, and a nitrogen-containing fragment is introduced into the system to synthesize a series of isopropanolamine-containing substructures and 1, 2, 3-triazole carbazole compounds; the compound has an excellent inhibition effect on plant pathogenic bacteria such as xanthomonas oryzae pv. Oryzae, xanthomonas axonopodis pv. Citri and Pseudomonas syringae pv.
Design, synthesis and biological activity evaluation of novel carbazole-benzylpiperidine hybrids as potential anti Alzheimer agents
Edraki, Najmeh,Faghih, Zeinab,Iraji, Aida,Nadri, Hamid,Rezaei, Zahra,Sadeghian, Batool,Sadeghian, Issa,Sakhteman, Amirhossein
, (2020/07/21)
Alzheimer's disease (AD) as the most common form of dementia in aged people, is an intricate neurodegenerative disease. Therefore, a novel strategy so-called multi-target-directed ligand has received much attention for the effective treatment of AD. In this study a series of novel carbazole-benzylpiperidine hybrids 9a-m was designed, synthesized and evaluated as acetylcholinesterase and butyrylcholinesterase inhibitors. Moreover, some of these compounds were evaluated for anti β-secretase (BACE1) activity and metal chelation properties. Among the synthesized compounds, compounds 9b (IC50 = 16.5 μM for AChE and IC50 = 0.59 μM for BuChE) and 9c (IC50 = 26.5 μM for AChE and IC50 = 0.18 μM for BuChE) showed the highest inhibitory activity against acetylcholinesterase and butyrylcholinesterase. Furthermore, these compounds (9b and 9c) displayed interaction with Zn2+ ion and compound 9c showed moderate inhibitory activity against BACE1 (24.5% at 50 μM). Kinetic and docking studies exhibited that these compounds likely act as a non-competitive inhibitor able to interact with the catalytic active site (CAS) and peripheral anionic site (PAS) of acetylcholinesterase simultaneously.
Identification of racemic and chiral carbazole derivatives containing an isopropanolamine linker as prospective surrogates against plant pathogenic bacteria: In vitro and in vivo assays and quantitative proteomics
Zhao, Yong-Liang,Huang, Xing,Liu, Li-Wei,Wang, Pei-Yi,Long, Qing-Su,Tao, Qing-Qing,Li, Zhong,Yang, Song
, p. 7512 - 7525 (2019/08/21)
Recent observations on the emergence of drug-resistant plant pathogenic bacteria have highlighted and elicited an acute campaign to develop novel, highly efficient antibiotic surrogates for managing bacterial diseases in agriculture. Thus, a type of racemic and chiral carbazole derivative containing an isopropanolamine pattern was systematically synthesized to discover low-cost and efficient antibacterial candidates. Screening results showed that compounds 2f, 6c, and 2j could significantly suppress the growth of tested plant pathogens, namely Xanthomonas oryzae pv oryzae, X. axonopodis pv citri, and Pseudomonas syringae pv actinidiae, and provided the corresponding EC50 values of 1.27, 0.993, and 0.603 μg/mL, which were significantly better than those of existing commercial drugs. In vivo studies confirmed their prospective applications for controlling plant bacterial diseases. Label-free quantitative proteomics analysis indicated that compound 2f could dramatically induce the up- and down-regulation of a total of 247 differentially expressed proteins, which was further validated by the parallel reaction monitoring technique. Moreover, fluorescence spectra and SEM images were obtained to further explore the antibacterial mechanism.
