- 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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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.
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Paragraph 0047; 0048
(2021/04/03)
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- Rational Optimization of 1,2,3-Triazole-Tailored Carbazoles As Prospective Antibacterial Alternatives with Significant in Vivo Control Efficiency and Unique Mode of Action
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Plant bacterial diseases can potentially damage agricultural products around the world, and few effective bactericides can manage these infections. Herein, to sequentially explore highly effective antibacterial alternatives, 1,2,3-triazole-tailored carbazoles were rationally fabricated. These compounds could suppress the growth of three main intractable pathogens including Xanthomonas oryzae pv oryzae (Xoo), X. axonopodis pv citri (Xac), and Pseudomonas syringae pv actinidiae (Psa) with lower EC50 values of 3.36 (3p), 2.87 (3p), and 4.57 μg/mL (3r), respectively. Pot experiments revealed that compound 3p could control the rice bacterial blight with protective and curative efficiencies of 53.23% and 50.78% at 200 μg/mL, respectively. Interestingly, the addition of 0.1% auxiliaries such as organic silicon and orange oil could significantly enhance the surface wettability of compound 3p toward rice leaves, resulting in improved control effectiveness of 65.50% and 61.38%, respectively. Meanwhile, compound 3r could clearly reduce the white pyogenic exudates triggered by Psa infection and afforded excellent control efficiencies of 79.42% (protective activity) and 78.74% (curative activity) at 200 μg/mL, which were quite better than those of commercial pesticide thiodiazole copper. Additionally, a plausible apoptosis mechanism for the antibacterial behavior of target compounds was proposed by flow cytometry, reactive oxygen species detection, and defensive enzyme (e.g., catalase and superoxide dismutase) activity assays. The current work can promote the development of 1,2,3-triazole-tailored carbazoles as prospective antibacterial alternatives bearing an intriguing mode of action.
- Huang, Xing,Liu, Hong-Wu,Long, Zhou-Qing,Li, Zhen-Xing,Zhu, Jian-Jun,Wang, Pei-Yi,Qi, Pu-Ying,Liu, Li-Wei,Yang, Song
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p. 4615 - 4627
(2021/05/06)
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- Design, synthesis and biological activity evaluation of novel carbazole-benzylpiperidine hybrids as potential anti Alzheimer agents
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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.
- Edraki, Najmeh,Faghih, Zeinab,Iraji, Aida,Nadri, Hamid,Rezaei, Zahra,Sadeghian, Batool,Sadeghian, Issa,Sakhteman, Amirhossein
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- Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel
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Aminoglycosides (AGs) are broad-spectrum antibiotics used for the treatment of serious bacterial infections but have use-limiting side effects including irreversible hearing loss. Here, we assessed the otoprotective profile of carvedilol in mouse cochlear cultures and in vivo zebrafish assays and investigated its mechanism of protection which, we found, may be mediated by a block of the hair cell's mechanoelectrical transducer (MET) channel, the major entry route for the AGs. To understand the full otoprotective potential of carvedilol, a series of 18 analogues were prepared and evaluated for their effect against AG-induced damage as well as their affinity for the MET channel. One derivative was found to confer greater protection than carvedilol itself in cochlear cultures and also to bind more tightly to the MET channel. At higher concentrations, both carvedilol and this derivative were toxic in cochlear cultures but not in zebrafish, suggesting a good therapeutic window under in vivo conditions.
- O'Reilly, Molly,Kirkwood, Nerissa K.,Kenyon, Emma J.,Huckvale, Rosemary,Cantillon, Daire M.,Waddell, Simon J.,Ward, Simon E.,Richardson, Guy P.,Kros, Corné J.,Derudas, Marco
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p. 5312 - 5329
(2019/06/07)
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- 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
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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.
- Zhao, Yong-Liang,Huang, Xing,Liu, Li-Wei,Wang, Pei-Yi,Long, Qing-Su,Tao, Qing-Qing,Li, Zhong,Yang, Song
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p. 7512 - 7525
(2019/08/21)
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- With chiral center carbazolyl isopropanolamine derivatives of the preparation method and application of (by machine translation)
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The invention relates to a with chiral center carbazolyl isopropanolamine derivatives of the preparation method and application. This compound has the general formula (I) indicated by the structure: The compound such as [...] Phaeosphaeria, tobacco wilt b
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Paragraph 0056; 0057; 0062; 0067
(2019/05/04)
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- Potential Antimicrobial Isopropanol-Conjugated Carbazole Azoles as Dual Targeting Inhibitors of Enterococcus faecalis
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A series of isopropanol-bridged carbazole azoles as potential antimicrobial agents were designed and synthesized from commercial carbazoles. Bioassay revealed that 3,6-dichlorocarbazolyl triazole 3f could effectively inhibit the growth of E. faecalis with minimal inhibitory concentration of 2 μg/mL. The active molecule 3f showed lower propensity to trigger the development of resistance in bacteria than norfloxacin and exerted rapidly bactericidal ability. Compound 3f also exhibited low cytotoxicity to normal mammalian RAW264.7 cells. Further mechanism exploration indicated that conjugate 3f was membrane active against E. faecalis and could form 3f-DNA complex by intercalating into DNA of resistant E. faecalis, which might be responsible for its antimicrobial action. Molecular docking showed an efficient binding of triazole derivative 3f with DNA gyrase enzyme through noncovalent interactions.
- Zhang, Yuan,Tangadanchu, Vijai Kumar Reddy,Cheng, Yu,Yang, Ren-Guo,Lin, Jian-Mei,Zhou, Cheng-He
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supporting information
p. 244 - 249
(2018/03/21)
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- Polymer dye-containing nanocomposites as photocatalysts
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A significant improvement of photocatalytic efficiency is achieved by the synthesis of TiO2/SiO2 nanocomposites where silica matrix provides the transport of reagents to TiO2 nanoparticles via porous structure, generation of the new active sites and thermal stability. The semiconductive films contained 10 or 30% of TiO2 in silica matrix are synthesized by sol-gel method using concentrated anatase titania colloid. The complex composites consisted of i) the Acridine Yellow dye molecules and the polyepoxypropyl carbazole; ii) the azobenzene containing polymer covered onto the titania/silica films are obtained as photocatalytic materials. Photocatalytic activity of the composites is tested via the reduction of dichromate ions.
- Linnik, Oksana,Nadtoka, Oksana
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p. 106 - 114
(2017/02/15)
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- Sulfonamido-derivatives of unsubstituted carbazoles as BACE1 inhibitors
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A novel series of variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylsulfonamides has been synthesized and assayed for β-Secretase (BACE1) inhibitory activity. BACE1 is a widely recognized drug target for the prevention and treatment of Alzheimer's Disease (AD). The introduction of benzyl substituents on the nitrogen atom of the arylsulfonamide moiety has so far led to the best results, with three derivatives showing IC50 values ranging from 1.6 to 1.9 μM. Therefore, a significant improvement over the previously reported series of N-carboxamides (displaying IC50's ≥ 2.5 μM) has been achieved, thus suggesting an active role of the sulfonamido-portion in the inhibition process. Preliminary molecular modeling studies have been carried out to rationalize the observed structure-activity relationships.
- Bertini, Simone,Ghilardi, Elisa,Asso, Valentina,Minutolo, Filippo,Rapposelli, Simona,Digiacomo, Maria,Saccomanni, Giuseppe,Salmaso, Veronica,Sturlese, Mattia,Moro, Stefano,Macchia, Marco,Manera, Clementina
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supporting information
p. 4812 - 4816
(2017/10/17)
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- Novel carbazole aminoalcohols as inhibitors of β-hematin formation: Antiplasmodial and antischistosomal activities
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Malaria and schistosomiasis are two of the most socioeconomically devastating parasitic diseases in tropical and subtropical countries. Since current chemotherapeutic options are limited and defective, there is an urgent need to develop novel antiplasmodials and antischistosomals. Hemozoin is a disposal product formed from the hemoglobin digestion by some blood-feeding parasites. Hemozoin formation is an essential process for the parasites to detoxify free heme, which is a reliable therapeutic target for identifying novel antiparasitic agents. A series of novel carbazole aminoalcohols were designed and synthesized as potential antiplasmodial and antischistosomal agents, and several compounds showed potent in?vitro activities against Plasmodium falciparum 3D7 and Dd2 strains and adult and juvenile Schistosoma japonicum. Investigations on the dual antiparasitic mechanisms showed the correlation between inhibitory activity of β-hematin formation and antiparasitic activity. Inhibiting hemozoin formation was identified as one of the mechanisms of action of carbazole aminoalcohols. Compound 7 displayed potent antiplasmodial (Pf3D7 IC50?=?0.248?μM, PfDd2 IC50?=?0.091?μM) and antischistosomal activities (100% mortality of adult and juvenile schistosomes at 5 and 10?μg/mL, respectively) and exhibited low cytotoxicity (CC50?=?7.931?μM), which could be considered as a promising lead for further investigation. Stoichiometry determination and molecular docking studies were also performed to explain the mode of action of compound 7.
- Wang, Weisi,Li, Qiang,Wei, Yufen,Xue, Jian,Sun, Xiao,Yu, Yang,Chen, Zhuo,Li, Shizhu,Duan, Liping
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p. 191 - 199
(2017/04/13)
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- Carbazole alkamine compound and preparation method thereof and application for parasitic disease resistance
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The invention provides a carbazole alkamine compound and a preparation method thereof and application for a parasitic disease resistance aspect. Specifically, the invention provides a racemic modification of the compound shown as type (A) and an enantiomer or salt capable of being accepted by pharmacy of the enantiomer. The compound has excellent anti-schistosoma and anti-hydatid cyst activity. According to the carbazole alkamine compound and the preparation method thereof and the application for the parasitic disease resistance aspect, the design is reasonable, the source of used raw materials is wide, the preparation method is easy and convenient and suitable for utility and can be applied to parasitic disease resistance drug preparation. Type A (please see the specifications for the chemical structural formula)
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Paragraph 0182; 0183; 0184; 0185; 0186
(2017/05/10)
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- Carbazole-containing sulfonamides and sulfamides: Discovery of cryptochrome modulators as antidiabetic agents
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A series of novel carbazole-containing sulfonamides and sulfamides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the results of efficacy studies in diet-induced obese (DIO) mice, and the desired pharmacokinetic parameters, compound 41 was selected for further profiling.
- Humphries, Paul S.,Bersot, Ross,Kincaid, John,Mabery, Eric,McCluskie, Kerryn,Park, Timothy,Renner, Travis,Riegler, Erin,Steinfeld, Tod,Turtle, Eric D.,Wei, Zhi-Liang,Willis, Erik
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p. 757 - 760
(2016/05/24)
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- Bromomethylthioindole Inspired Carbazole Hybrids as Promising Class of Anti-MRSA Agents
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Series of N-substituted carbazole analogues bearing an indole ring were synthesized as anti-methicillin-resistant Staphylococcus aureus (MRSA) agents from a molecular hybridization approach. The representative compound 19 showed an MIC = 1 μg/mL against a panel of MRSA clinical isolates as it possessed comparable in vitro activities to that of vancomycin. Moreover, compound 19 also exhibited MIC = 1 μg/mL activities against a recent identified Z172 MRSA strain (vancomycin-intermediate and daptomycin-nonsusceptible phenotype) and the vancomycin-resistant Enterococcus faecalis (VRE) strain. In a mouse model with lethal infection of MRSA (4N216), a 75% survival rate was observed after a single dose of compound 19 was intravenously administered at 20 mg/kg. In light of their equipotent activities against different MRSA isolates and VRE strain, the data underscore the importance of designed hybrid series for the development of new N-substituted carbazoles as potential anti-MRSA agents.
- Cheng, Chia-Yi,Chang, Chun-Ping,Lauderdale, Tsai-Ling Yang,Yu, Guann-Yi,Lee, Jinq-Chyi,Jhang, Yi-Wun,Wu, Chien-Huang,Ke, Yi-Yu,Sadani, Amit A.,Yeh, Ching-Fang,Huang, I-Wen,Kuo, Yi-Ping,Tsai, De-Jiun,Yeh, Teng-Kuang,Tseng, Chen-Tso,Song, Jen-Shin,Liu, Yu-Wei,Tsou, Lun K.,Shia, Kak-Shan
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supporting information
p. 1191 - 1196
(2016/12/18)
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- Synthesis and biological evaluation of novel 1,2,4-triazine derivatives bearing carbazole moiety as potent α-glucosidase inhibitors
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A new series of 1,2,4-triazine derivatives bearing carbazole moiety 7a-7p were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent α-glucosidase inhibitory activity, with IC50 values in the range of 4.27 ± 0.07-47.75 ± 0.25 μM as compared to the standard drug acarbose. Among the series, compound 7k represented the most potent α-glucosidase inhibitory activity with IC50 values of 4.27 ± 0.07 μM. Kinetic analysis revealed that compound 7k is a non-competitive inhibitor with a Ki of 4.43 μM. Furthermore, the binding interactions of compound 7k with α-glucosidase was confirmed through molecular docking. This study showed these 1,2,4-triazine derivatives bearing carbazole moiety as a new class of α-glucosidase inhibitors.
- Wang, Guangcheng,Wang, Jing,He, Dianxiong,Li, Xin,Li, Juan,Peng, Zhiyun
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p. 2806 - 2809
(2016/06/09)
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- Carbazole Aminoalcohols Induce Antiproliferation and Apoptosis of Human Tumor Cells by Inhibiting Topoisomerase I
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Novel carbazole aminoalcohols were designed and synthesized as anticancer agents. Among them, alkylamine-chain-substituted compounds showed the most promising antiproliferative activity, with IC50values in the single-digit micromolar range against two human tumor cell lines. Topoisomerase I (topo I) is likely to be one of the targets of these compounds. Results of comet assays and molecular docking indicate that the representative compounds may act as topo I poisons, causing single-strand DNA damage by stabilizing the topo I–DNA cleavage complex. In particular, the most potent compound, 1-(butylamino)-3-(3,6-dichloro-9H-carbazol-9-yl)propan-2-ol (6), was shown to be able to induce G2-phase cell-cycle arrest and apoptosis in HeLa cells.
- Wang, Weisi,Sun, Xiao,Sun, Deheng,Li, Shizhu,Yu, Yang,Yang, Tingyuan,Yao, Junmin,Chen, Zhuo,Duan, Liping
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p. 2675 - 2681
(2016/12/23)
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- CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS
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The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
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Paragraph 0272
(2015/10/28)
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- Computer-aided structure-based design of multitarget leads for Alzheimer's disease
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Alzheimer's disease is a neurodegenerative pathology with unmet clinical needs. A highly desirable approach to this syndrome would be to find a single lead that could bind to some or all of the selected biomolecules that participate in the amyloid cascade, the most accepted route for Alzheimer disease genesis. In order to circumvent the challenge posed by the sizable differences in the binding sites of the molecular targets, we propose a computer-assisted protocol based on a pharmacophore and a set of required interactions with the targets that allows for the automated screening of candidates. We used a combination of docking and molecular dynamics protocols in order to discard nonbinders, optimize the best candidates, and provide a rationale for their potential as inhibitors. To provide a proof of concept, we proceeded to screen the literature and databases, a task that allowed us to identify a set of carbazole-containing compounds that initially showed affinity only for the cholinergic targets in our experimental assays. Two cycles of design based on our protocol led to a new set of analogues that were synthesized and assayed. The assay results revealed that the designed inhibitors had improved affinities for BACE-1 by more than 3 orders of magnitude and also displayed amyloid aggregation inhibition and affinity for AChE and BuChE, a result that led us to a group of multitarget amyloid cascade inhibitors that also could have a positive effect at the cholinergic level.
- Domnguez, Jos L.,Fernndez-Nieto, Fernando,Castro, Marian,Catto, Marco,Paleo, M. Rita,Porto, Silvia,Sardina, F. Javier,Brea, Jos M.,Carotti, Angelo,Villaverde, M. Carmen,Sussman, Fredy
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p. 135 - 148
(2015/02/05)
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- Membrane-targeting dcap analogues with broad-spectrum antibiotic activity against pathogenic bacteria
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We performed a structure-activity relationship study of 2-((3-(3,6-dichloro-9H-carbazol-9-yl)-2-hydroxypropyl)amino)-2-(hydroxymethyl)propane-1,3-diol (DCAP), which is an antibacterial agent that disrupts the membrane potential and permeability of bacteri
- Hurley, Katherine A.,Heinrich, Victoria A.,Hershfield, Jeremy R.,Demons, Samandra T.,Weibel, Douglas B.
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supporting information
p. 466 - 471
(2015/04/27)
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- Carbazole-Containing Sulfonamides as Cryptochrome Modulators
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The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.
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Paragraph 0254-0255
(2013/11/19)
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- Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors
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A library of 1,3-disubstituted 2-propanols was synthesized and evaluated as low molecular weight probes for β-secretase inhibition. By screening a library of 121 1,3-disubstituted 2-propanol derivatives, we identified few compounds inhibiting the enzyme at low micromolar concentrations. The initial hits were optimized to yield a potent BACE-1 inhibitor exhibiting an IC 50 constant in the nanomolar range. Exploration of the pharmacological properties revealed that these small molecular inhibitors possessed a high selectivity over cathepsin D and desirable physicochemical properties beneficial to cross the blood-brain barrier.
- Kumar, Arun Babu,Anderson, Jordan Micheal,Melendez, Anthony Lester,Manetsch, Roman
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supporting information; experimental part
p. 4740 - 4744
(2012/08/07)
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- Carbazole-containing arylcarboxamides as BACE1 inhibitors
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β-Secretase (BACE1) is widely recognized as a prime drug target for the treatment of Alzheimer's disease (AD). In this Letter, we report the synthesis and the BACE1 inhibitory activity of novel, variously substituted N-[3-(9H-carbazol-9-yl)-2-hydroxypropyl]-arylcarboxamides. The best results have been obtained with the introduction of a 4-OMe substituent (IC50 = 3.8 μM) or a 3,4-dichloro substituent (IC50 = 2.5 μM) in the amidic aromatic ring. The blood-brain barrier penetration predictions resulted to be promising for this type of compounds. To better understand the structure-activity relationships (SAR) of the new derivatives, a docking study procedure has been applied exploiting different conformational and ionic states of BACE1.
- Bertini, Simone,Asso, Valentina,Ghilardi, Elisa,Granchi, Carlotta,Manera, Clementina,Minutolo, Filippo,Saccomanni, Giuseppe,Bortolato, Andrea,Mason, Jonathan,Moro, Stefano,MacChia, Marco
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scheme or table
p. 6657 - 6661
(2011/12/04)
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- Synthesis of 9-substituted 2,3,4,9-tetrahydro-1H-carbazole derivatives and evaluation of their anti-prion activity in TSE-infected cells
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2,3,4,9-Tetrahydro-9-[2-hydroxy-3-(1-piperidinyl)propyl] -6-methyl-1H-carbazol-1-one (GJP14) is a novel anti-prion compound that we previously discovered by in silico screening and cellular assay. In this study, a variety of GJP14 derivatives were prepared using pyrrole derivatives, (haloalkyl)oxiranes, and amines, and their anti-prion activity was evaluated in TSE-infected cells. It was found that the tricyclic aromatic ring, a hydroxy group at the 2-position and an amino group at the 3-position of the N-propyl group were the basic requirements for anti-prion activity. The derivatives bearing an N-ortho-halobenzyl group exhibited an improved activity, and the most potent derivative was 8 times as effective as the original lead compound, GJP14.
- Kimura, Tsutomu,Hosokawa-Muto, Junji,Asami, Kenji,Murai, Toshiaki,Kuwata, Kazuo
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supporting information; experimental part
p. 5675 - 5679
(2012/01/02)
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- Structure-activity relationship studies of the chromosome segregation inhibitor, Incentrom A
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A series of Incentrom A analogs that inhibit the chromosome segregation process in yeast were synthesized and tested for their effects on chromosome stability and cell proliferation. Pharmacophore and structure-activity relationship of Incentrom A for the anti-yeast activity were established.
- Lee, Hee-Yoon,Jung, Yongsik,Kim, Wonyeob,Kim, Jin Hee,Suh, Min-Soo,Shin, Seung Koo,Yoon, Hye-Joo
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scheme or table
p. 4670 - 4674
(2009/04/08)
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- Enantioselective incorporation of carbon dioxide into epoxides catalyzed by optically active cobalt(II) complexes
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The enantioselective chemical fixation of CO2 into an epoxide was developed using an optically active ketoimi-natocobalt(II) complex as a chiral Lewis acid. In the presence of a catalytic amount of the cobalt complex and amine base, enantioselective CO2 fixation with an epoxide proceeded with kinetic resolution to afford the corresponding carbonate along with unreacted epoxide, both of which were optically active. To improve their enantioselectivities, the ligand structures of the cobalt complexes and amine bases were examined. Thus, the optimized catalytic system was successfully applied to various epoxides to obtain the corresponding optically active cyclic carbonates and to recover epoxides with good-to-high enantioselectivities.
- Yamada, Wataru,Kitaichi, Yasunori,Tanaka, Hirotaka,Kojima, Tomohide,Sato, Mitsuo,Ikeno, Taketo,Yamada, Tohru
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experimental part
p. 1391 - 1401
(2009/06/20)
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- Diols with carbazole ring and their aza derivatives
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Diols with carbazole ring were obtained in reactions of 9-(2-chloroethyl)carbazole with excess of diethanolamine and 9-(2,3-epoxypropyl)carbazole with water or ethylene glycol. These diols were derivatized into aza compounds by the reactions with aromatic
- Lubczak, Renata
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p. 201 - 208
(2007/10/03)
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- Microwave-assisted epoxidation of simple alkenes in the presence of hydrogen peroxide
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A novel application of microwave irradiation for the epoxidation of some simple alkenes, in which hydrogen peroxide was used as an oxidant together with sodium tungsten and phosphorous acid under phase-transfer catalytic (PTC) conditions, is described as a new environmentally benign method. In comparison with conventional heating, the microwave process is a very useful alternative for introducing of the oxirane ring into some unsaturated hydrocarbons because of reduction of the reaction time and increase in yield. Copyright Taylor & Francis, Inc.
- Bogdal,Lukasiewicz,Pielichowski,Bednarz
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p. 2973 - 2983
(2007/10/03)
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