329-59-9Relevant academic research and scientific papers
Regioselective Synthesis of Angular Isocoumarinselenazoles: A Benzoselenazole-directed, Site-specific, Ruthenium-catalyzed C(sp2)-H Activation
Dhole, Sandip,Liao, Jen-Yu,Kumar, Sunil,Salunke, Deepak B.,Sun, Chung-Ming
, p. 942 - 950 (2018)
The synthesis of new, angular isocoumarinselenazoles is described, which involves the construction of 2-amino benzoselenazoles and their regioselective C2N-alkylation and alkyne insertion. An expeditious and metal-free synthesis of 2-aminobenzoselenazoles
PGDH INHIBITORS AND METHODS OF MAKING AND USING
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Paragraph 0271; 0278-0279, (2021/07/31)
Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.
Preparation method of 3-acetylindole BRPF1 inhibitor and use of 3-acetylindole BRPF1 inhibitor
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Paragraph 0077-0080; 0134-0136, (2020/03/03)
The invention relates to a 3-acetylindole compound of a novel structure shown in a formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate or a solvate thereof, a preparation method of the compound, a pharmaceutical composition containing a therapeutically effective dose of the compound, and use thereof as a protein tyrosine kinase inhibitor, especially as a bromine-containing area PHD zinc finger protein 1 (BRPF1) inhibitor, in the prevention or treatment of disease benefited from the inhibition of BRPF1.
Benzimidazole derivatives as potent and isoform selective tumor-associated carbonic anhydrase IX/XII inhibitors
?al??kan, Burcu,Banoglu, Erden,Gür Maz, Tu??e,Nocentini, Alessio,Supuran, Claudiu T.,Uslu, Azize Gizem
supporting information, (2020/01/08)
We describe the synthesis of a series of 2-arylbenzimidazole derivatives bearing sulfonamide functionality (4a–d, 7a–c and 10) as well as hydroxamic acid (15a–b), carboxylic acid (16a–b), carboxamide (17a–b) and boronic acid (22a–b and 26) functionalities, which act as human carbonic anhydrase (hCA, EC 4.2.1.1) inhibitors. The newly synthesized benzimidazole derivatives were evaluated against 4 physiologically relevant CA isoforms (hCA I, II, IX, and XII), and especially the sulfonamide-containing benzimidazoles demonstrated intriguing inhibitory activity against tumor associated CA IX and XII with KI values in the range of 5.2–29.3 nM and 9.9–41.7 nM, respectively. Notably, compound 4c was the most potent and selective CA IX (KI = 6.6 nM) and XII (KI = 9.9 nM) inhibitor with a significant selectivity ratio over cytosolic CA I and II isoforms in the range of 3.4–25.2. In addition, compounds having hydroxamic acid (15a-b) or carboxylic acid (16a-b) functionalities resulted in greater selectivity ratios for CA IX/XII over CAI/II in the range of 4.1–121.5 although with KI values in lower micromolar potency (KIs = 0.36–0.85 μM for CA IX/XII).
EXON SKIPPING OLIGOMER CONJUGATES FOR MUSCULAR DYSTROPY
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Paragraph 0379, (2020/07/07)
Antisense oligomers complementary to a selected target site in the human dystrophin gene to induce exon 50 skipping are described. In various aspects, antisense oligomers are described according to Formula (I): or a pharmaceutically acceptable salt thereo
Substituent effects on the isomerization of hydrazone switches driven by the intramolecular hydrogen bond
Lu, Chaocao,Htan, Bu,Fu, Shitao,Ma, Chunmiao,Gan, Quan
, p. 4010 - 4016 (2019/07/03)
In this work, the substituent effects on hydrogen bonding in one kind of hydrazone-based switch are revealed. The E/Z isomerization ratios of these hydrazones and their intramolecular hydrogen bond strengths in the Z form were evaluated using NMR technique. Linear correlations between these parameters and Hammett empirical values for substituent effects are explored as well.
PROCESSES FOR PREPARING PHOSPHORODIAMIDATE MORPHOLINO OLIGOMERS VIA FAST-FLOW SYNTHESIS
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Page/Page column 80-81, (2019/04/16)
Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.
MODULATORS OF ORPHAN NUCLEAR RECEPTORS FOR NASH AND OTHER METABOLIC DISORDERS
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Page/Page column 58-60, (2019/11/19)
Compounds, compositions and methods for modulating retinoic acid receptor-like orphan receptors (ROR) and associated diseases. Methods for treatment or prophylaxis of metabolic disorders, liver disorders or diseases, including NASH, immune disorders, cent
Oridonin derivatives as potential anticancer drug candidates triggering apoptosis through mitochondrial pathway in the liver cancer cells
Luo, Dongdong,Yi, Yujiao,Peng, Kai,Liu, Tangrong,Yang, Jiayu,Liu, Shan,Zhao, Wanzhou,Qu, Xianjun,Yu, Wengong,Gu, Yuchao,Wan, Shengbiao
, p. 365 - 379 (2019/06/17)
The biological function of the natural ent-kaurene diterpenoid isolated from genus Isodon, oridonin, has been intensively studied. However, its mechanism studies and clinical applications were hampered by its moderate biological activities. In order to en
SUBSTITUTED 2-AMINOBENZIMIDAZOLES ANALOGS AS ANTIBIOFILM AGENTS
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Paragraph 0225; 0226; 0237, (2019/10/29)
In one aspect, the disclosure relates to compositions and methods for dispersing exiting Salmonella biofilms and inhibiting formation of Salmonella biofilms. In various aspects, the disclosed compositions can be used in methods of treating a persistent Sa
