17450-29-2Relevant academic research and scientific papers
A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects
Zhou, Jie,Cai, Xingguang,Huang, Xun,Dai, Yuxuan,Sun, Lidan,Zhang, Bo,Yang, Bo,Lin, Haiyan,Huang, Wenlong,Qian, Hai
, p. 1158 - 1169 (2017)
Glucagon has plenty of effects via a specific glucagon receptor(GCGR) like elevating the blood glucose, improving fatty acids metabolism, energy expenditure and increasing lipolysis in adipose tissue. The most important role of glucagon is to regulate the blood glucose, but the emergent possibilities of hyperglycaemia is exist. Glucagon could also slightly activate glucagon-like peptide-1 receptor(GLP-1R), which lead to blood glucose lowering effect. This study aims to erase the likelihood of hyperglycaemia and to remain the inherent catabolic effects through improving GLP-1R activation and deteriorating GCGR activation so as to lower the bodyweight and show diabetes-protective effects. Firstly, twelve cysteine modified GLP-1/GCGR dual agonists were synthesized (1–12). Then, the GLP-1R/GCGR mediated activation and biological activity in normal ICR mice were comprehensively performed. Compounds substituted by cysteine at positions 22, 23 and 25 in glucagon were observed to be better regulators of the body weight and blood glucose. To prolong the half-lives of derivatives, various fatty side chain maleimides were modified to optimal glucagon analogues. Laurate maleimide conjugate 4d was the most potent. Administration of 1000 nmol/kg 4d once every two days for a month normalized adiposity and glucose tolerance in diet-induced obese (DIO) mice. Improvements in plasma metabolic parameters including insulin, leptin, and adiponectin were observed. These studies suggest that compound 4d behaves well in lowering body weight and maintaining energy expenditure without a chance of hyperglycaemia, 4d has strong clinical potential as an efficient GLP-1/GCGR agonist in the prevention and treatment of obesity and dyslipidemia.
Chemically Delaminated Free-Standing Ultrathin Covalent Organic Nanosheets
Khayum, M. Abdul,Kandambeth, Sharath,Mitra, Shouvik,Nair, Sanoop B.,Das, Anuja,Nagane, Samadhan S.,Mukherjee, Rabibrata,Banerjee, Rahul
, p. 15604 - 15608 (2016)
Covalent organic nanosheets (CONs) are a new class of porous thin two-dimensional (2D) nanostructures that can be easily designed and functionalized and could be useful for separation applications. Poor dispersion, layer restacking, and difficult postsynthetic modifications are the major hurdles that need to be overcome to fabricate scalable CON thin films. Herein, we present a unique approach for the chemical exfoliation of an anthracene-based covalent organic framework (COF) to N-hexylmaleimide-functionalized CONs, to yield centimeter-sized free-standing thin films through layer-by-layer CON assembly at the air–water interface. The thin-layer fabrication technique presented here is simple, scalable, and does not require any surfactants or stabilizing agents.
One-Pot Double-Annulation Strategy for the Synthesis of Unusual Fused Bis-Heterocycles
Abdul-Rashed, Shukree,Alachouzos, Georgios,Brennessel, William W.,Frontier, Alison J.
supporting information, p. 4350 - 4354 (2020/06/04)
A novel metal-free double-annulation cascade for the construction of unusual fused heterocyclic systems is described. This simple protocol enables the sequential assembly of two rings in one pot from two simple precursors. Acidic conditions promote the condensation and the intramolecular alkynyl Prins reaction of an enyne or arenyne alcohol with a cyclic hemiaminal to form a five-, six-, or seven-membered oxacycle followed by a seven-or eight-membered azacycle. In this transformation, chemical complexity is rapidly generated with the formation of three new bonds (one C-O, one C-C, and one C-N) in one synthetic operation. The strategy is modular and relatively general, providing access to a series of unique fused bicyclic scaffolds.
Anti-leishmanial and cytotoxic activities of a series of maleimides: Synthesis, biological evaluation and structure-activity relationship
Fan, Yongxian,Lu, Yuele,Chen, Xiaolong,Tekwani, Babu,Li, Xing-Cong,Shen, Yinchu
, (2018/11/24)
In the present study, 45 maleimides have been synthesized and evaluated for anti-leishmanial activities against L. donovani in vitro and cytotoxicity toward THP1 cells. All compounds exhibited obvious anti-leishmanial activities. Among the tested compounds, there were 10 maleimides with superior anti-leishmanial activities to standard drug amphotericin B, and 32 maleimides with superior anti-leishmanial activities to standard drug pentamidine, especially compounds 16 (IC50 50 50 > 10 μg/mL). The anti-leishmanial activities of 16 and 42 were 10 times better than that of amphotericin B. The structure and activity relationship (SAR) studies revealed that 3,4-non-substituted maleimides displayed the strongest anti-leishmanial activities compared to those for 3-methyl-maleimides and 3,4-dichloro-maleimides. 3,4-dichloro-maleimides were the least cytotoxic compared to 3-methyl-maleimides and 3,4-non-substituted maleimides. The results show that several of the reported compounds are promising leads for potential anti-leishmanial drug development.
BENZOBIS-(THIADIAZOLE) DERIVATIVE, INK CONTAINING THE SAME, AND ORGANIC ELECTRONICS DEVICE USING THE SAME
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Paragraph 0293; 0298; 0299; 0300; 0301, (2016/10/08)
The object of the present invention is to provide a benzobis-(thiadiazole) derivative which has excellent electron mobility (field-effect mobility) and excellent stability in the atmosphere. The present invention relates to a benzobis-(thiadiazole) derivative which has a cyclic imide structure with condensed aromatic ring in its molecule shown in the formula (1) or (2): (In the formula, R, A and Z represent specific groups.)
Functionalized phosphonated half-cage molecules as ligands for metal complexes
Villemin, Elise,Herent, Marie-France,Marchand-Brynaert, Jacqueline
supporting information, p. 6165 - 6178 (2013/01/15)
Phosphonated molecules, featuring a half-cage structure and a N-lateral chain with additional metal coordinating groups were designed as ligands of metal cations. These compounds were synthesized by a Diels-Alder (DA) strategy, using 1-diethoxyphosphoryl-1,3-butadiene and a series of N-substituted maleimides as dienophiles. Two cycloadducts, bearing a terminal primary alcohol and a terminal iodide, respectively, were used as key intermediates for further functionalizations. Metal coordination properties of the ligands equipped with functionalized N-lateral chains were proven by an ESI-HRMS study. The stoichiometry of one selected EuIII complex with a diphosphonated ligand was determined by photoluminescence spectroscopy in emission mode.
MYCOBACTERIAL INHIBITORS
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Page/Page column 9, (2010/11/08)
The invention provides the use of certain succinimide compounds in the treatment of mycobacterial diseases.
3-Azabicyclo[3.1.0]hexane derivatives useful in therapy
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, (2008/06/13)
Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.
Design, Synthesis, and in Vitro Activity of Bis(succinimido)hexane Peptide Heterodimers with Combined B1 and B2 Antagonist Activity
Cheronis, John C.,Whalley, Eric T.,Allen, Lisa G.,Loy, Sharon D.,Elder, Megan W.,et al.
, p. 348 - 355 (2007/10/02)
We have developed a series of peptide heterodimers based on the B2 antagonist D-Arg0-3,D-Phe7,Leu8>-BK (1) and the B1 antagonist Lys0-8,des-Arg9>-BK
Process for preparation of N-substituted maleimides
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, (2008/06/13)
N-substituted maleimide represented by formula (2): STR1 is produced from N-substituted maleamic acid monoester represented by formula (1): STR2 in the presence of an acid catalyst by elmination of an alcohol from the monoester. The above N-substituted maleamic acid monoester represented by formula (1) is produced by esterification of N-substituted maleamic acid represented by formula (3): STR3 with an alcohol R2 -OH in the represence of an acid catalyst.
