56674-88-5Relevant academic research and scientific papers
Adamantane 11-β-HSD-1 inhibitors: Application of an isocyanide multicomponent reaction
Sorensen, Bryan,Rohde, Jeff,Wang, Jiahong,Fung, Steven,Monzon, Katina,Chiou, William,Pan, Liping,Deng, Xiaoqing,Stolarik, DeAnne,Frevert, Ernst U.,Jacobson, Peer,Link
, p. 5958 - 5962 (2006)
A series of potent and selective adamantane aminoamide 11-β-HSD-1 inhibitors has been optimized. Chemically these studies were expedited by utilizing readily obtained amino acids as starting materials or an isocyanide multicomponent reaction. Structure-ac
A Robust Au?C≡C Functionalized Surface: Toward Real-Time Mapping and Accurate Quantification of Fe2+ in the Brains of Live AD Mouse Models
Liao, Fumin,Liu, Zhichao,Tian, Yang,Wan, Jingjing,Zhang, Chuanping,Zhang, Limin,Zhou, Jian,Zhu, Anwei
, p. 20499 - 20507 (2020)
Described here is that Au?C≡C bonds showed the highest stability under biological conditions, with abundant thiols, and the best electrochemical performance compared to Au?S and Au?Se bonds. The new finding was also confirmed by theorical calculations. Based on this finding, a specific molecule for recognition of Fe2+ was designed and synthesized, and used to create a selective and accurate electrochemical sensor for the quantification of Fe2+. The present ratiometric strategy demonstrates high spatial resolution for real-time tracking of Fe2+ in a dynamic range of 0.2–120 μM. Finally, a microelectrode array with good biocompatibility was applied in imaging and biosensing of Fe2+ in the different regions of live mouse brains. Using this tool, it was discovered that the uptake of extracellular Fe2+ into the cortex and striatum was largely mediated by cyclic adenosine monophosphate (cAMP) through the CREB-related pathway in the brain of a mouse with Alzheimer's disease.
TRIOXOLANE AGENTS
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Paragraph 0425; 0426, (2019/01/16)
Disclosed herein, inter alia, are trioxolane compounds and methods of using the same for treatment and detection of diseases.
Activity-based protein profiling reveals that secondary-carbon-centered radicals of synthetic 1,2,4-trioxolanes are predominately responsible for modification of protein targets in malaria parasites
Wei, Chunyan,Zhao, Cheng-Xiao,Liu, Sheng,Zhao, Jin-Hui,Ye, Zi,Wang, Heng,Yu, Shi-Shan,Zhang, Chong-Jing
, p. 9535 - 9538 (2019/08/15)
Endoperoxide-containing antimalarials, such as artemisinin and the synthetic trioxolane OZ439, are prodrugs activated by heme to generate primary and secondary carbon-centered radicals. We employed activity-based protein profiling (ABPP) to show that the
CARBOXYLATE, CARBOXYLIC ACID GENERATOR, RESIST COMPOSITION, AND METHOD FOR PRODUCING RESIST PATTERN
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Paragraph 0213, (2018/09/30)
PROBLEM TO BE SOLVED: To provide a salt and a resist composition capable of producing a resist pattern having a good mask error factor. SOLUTION: A carboxylate represented by formula (I), an acid generator containing the carboxylate, and a resist composition containing the acid generator are provided. [In the formula, Xa and Xb each independently represent an oxygen atom or a sulfur atom; X1 represents a hydrocarbon group which may have a substituent; L1 and L2 each independently represent a single bond or a hydrocarbon group which may have a substituent; R1 and R2 each independently represent an alicyclic hydrocarbon group which may have a substituent; -CH2- contained in the hydrocarbon groups and the alicyclic hydrocarbon group may be substituted with -O-, -S-, -CO-, or -S(O)2-; and Z1+ represents an organic cation.] SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
A click chemistry-based proteomic approach reveals that 1,2,4-trioxolane and artemisinin antimalarials share a common protein alkylation profile
Ismail, Hanafy M.,Barton, Victoria E.,Panchana, Matthew,Charoensutthivarakul, Sitthivut,Biagini, Giancarlo A.,Ward, Stephen A.,O'Neill, Paul M.
supporting information, p. 6401 - 6405 (2016/06/01)
In spite of the recent increase in endoperoxide antimalarials under development, it remains unclear if all these chemotypes share a common mechanism of action. This is important since it will influence cross-resistance risks between the different classes. Here we investigate this proposition using novel clickable 1,2,4-trioxolane activity based protein-profiling probes (ABPPs). ABPPs with potent antimalarial activity were able to alkylate protein target(s) within the asexual erythrocytic stage of Plasmodium falciparum (3D7). Importantly, comparison of the alkylation fingerprint with that generated from an artemisinin ABPP equivalent confirms a highly conserved alkylation profile, with both endoperoxide classes targeting proteins in the glycolytic, hemoglobin degradation, antioxidant defence, protein synthesis and protein stress pathways, essential biological processes for plasmodial survival. The alkylation signatures of the two chemotypes show significant overlap (ca. 90 %) both qualitatively and semi-quantitatively, suggesting a common mechanism of action that raises concerns about potential cross-resistance liabilities. Clickable 1,2,4-trioxolane activity-based protein-profiling probes (ABPPs) were designed to retain antimalarial activity and alkylate the molecular targets of the blood stage of Plasmodium falciparum in situ. Comparison of the 1,2,4-trioxolane protein alkylation signature with the corresponding artemisinin ABPPs indicates that both drug classes target key proteins in the glycolytic, hemoglobin degradation, antioxidant defence and protein synthesis pathways.
NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0065; 0066, (2015/05/06)
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
ATX MODULATING AGENTS
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Page/Page column 173, (2015/12/24)
Compounds of formula (I) can modulate the activity of autotaxin (ATX).
NOVEL COMPOUND HAVING ABILITY TO INHIBIT 11B-HSD1 ENZYME OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
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Paragraph 0424-0426, (2015/08/04)
The present invention relates to a novel compound or a pharmaceutically acceptable salt thereof inhibiting 11β-HSD1 enzyme activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. Since the compound of the present invention selectively inhibits the activity of 11β-HSD1 (11β-Hydroxysteroid dehydrogenase type 1), the compound of the invention can be effectively used as a therapeutic agent for the treatment of diseases caused by the over-activation of 11β-HSD1 such as non-insulin dependent type II diabetes, insulin resistance, obesity, lipid disorder, metabolic syndrome, and other diseases or condition mediated by the excessive activity of glucocorticoid.
Selective trioxolane based bifunctional molecular linkers for covalent heme surface functionalisation
McConville,Bradley,Zhou,Schiffrin,O'Neil
, p. 186 - 188 (2014/01/06)
A bifunctional molecular linker containing both aryl diazonium and trioxolane groups was synthesised and its ability to sequentially functionalise glassy carbon and covalently immobilise heme investigated. Functionalisation was demonstrated by electrochemical techniques.
