21451-32-1Relevant articles and documents
Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis
Bao, Xuefei,Chen, Guoliang,Du, Fangyu,Hammock, Bruce D.,Liu, Qiu,Liu, Zhongbo,Morisseau, Christophe,Sun, Wenjiao,Wang, Chao,Xiao, Wei,Yang, Hao,Zhang, Tan,Zhou, Jun
, (2021/07/06)
Sepsis, a systemic inflammatory response, caused by pathogenic factors including microorganisms, has high mortality and limited therapeutic approaches. Herein, a new soluble epoxide hydrolase (sEH) inhibitor series comprising a phenyl ring connected to a
Succinamide derivatives ameliorate neuroinflammation and oxidative stress in scopolamine-induced neurodegeneration
Anwar, Tayyaba,Ashraf, Zaman,Imran, Muhammad,Iqbal, Sumbal,Khan, Tariq,Li, Shupeng,Nadeem, Humaira,Naeem, Komal,Sarwar, Sadia,Shah, Fawad Ali
, (2020/04/10)
Oxidative stress-mediated neuroinflammatory events are the hallmark of neurodegenerative diseases. The current study aimed to synthesize a series of novel succinamide derivatives and to further investigate the neuroprotective potential of these compounds
COMPOUND AND THERMOPLASTIC RESIN COMPOSITION AND MOLDED ARTICLE CONTAINING THE SAME
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Paragraph 0090-0092, (2020/11/03)
PROBLEM TO BE SOLVED: To provide a compound having a high cost performance capable of imparting significant crystallization accelerating action to a thermoplastic resin even with a small amount of addition, an additive for a thermoplastic resin, an additi
Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity
Kam, Yoo Lim,Rhee, Hee-Kyung,Kim, Hwa-Jung,Back, Seung Keun,Na, Heung Sik,Choo, Hea-Young Park
experimental part, p. 2327 - 2336 (2010/05/18)
A series of novel non-peptide diamide compounds was synthesized and evaluated as antibradykinin agents by utilizing guinea-pig ileum smooth muscle. Among the final compounds, (Z)-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-4-oxo-N-(4-phenylbutan-2-yl)
Atypical oxidation reaction by thionyl chloride: Easy two-step synthesis of N-alkyl-1,4-dithiines
Valla, Alain,Cartier, Dominique,Zentz, Frederic,Labia, Roger
, p. 3591 - 3597 (2007/10/03)
Easy two-step synthesis of a series of dithiines was performed from succinic anhydride via cyclization of the corresponding 4-(alkylamino)-4- oxobutanoic acids (succinamic acids). The reaction, carried out in polar aprotic solvents, gave 4,8-dithiine-indacene-1,3,5,7-tetraones (diimides 3) via 3,7-bis-4,8-dithia-indacene-1,5-diones (diisoimides 2), which could be isolated. Surprisingly, in this reaction, thionyl chloride appeared as an oxidant, and this process seemed to be useful for the syntheses of S-containing heterocyclic compounds such as 1,4-dithiins. A mechanistic pathway was considered. Copyright Taylor & Francis Group, LLC.
Syntheses, in vitro antibacterial and antifungal activities of a series of N-alkyl, 1,4-dithiines
Zentz,Labia,Sirot,Faure,Grillot,Valla
, p. 944 - 947 (2008/09/18)
A series of dithiines were synthesized by cyclization of 4-(alkylamino)-4-oxobutanoic acids under the action of SOCl2. Their in vitro antibacterial and antifungal activities have been evaluated against reference strains and versus reference compounds. The so-called 'isoimides' 2a, 2b were totally inactive whereas some imides had low MICs for few bacteria and for few fungal microorganisms.
Facile syntheses and characterization of hyperbranched poly(ester-amide)s from commercially available aliphatic carboxylic anhydride and multihydroxyl primary amine
Li, Xiuru,Zhan, Jie,Li, Yuesheng
, p. 7584 - 7594 (2007/10/03)
A new method for synthesis of novel hyperbranched poly(ester-amide)s from commercially available AA′ and CBx type monomers has been developed on the basis of a series of model reactions. The hyperbranched poly(ester-amide)s with multihydroxyl end groups are prepared by thermal polycondensation of carboxyl anhydrides (AA′) and multihydroxyl primary amine (CBx) without any catalyst and solvent. The reaction mechanism in the initial stage of polymerization was investigated with in situ 1H NMR. In the initial stage of the reaction, primary amino groups of 2-amino-2-ethyl-1,3-propanediol (AEPO) or tris(hydroxymethyl)aminomethane (THAM) react rapidly with anhydride, forming an intermediate which can be considered as a new ABx type monomer. Further self-polycondensation reactions of the ABx molecules produce hyperbranched polymers. Analysis using 1H and 13C NMR spectroscopy revealed the degree of branching of the resulting polymers ranging from 0.36 to 0.55. These hyperbranched poly(ester-amide)s contain configurational isomers observed by 13C and DEPT 13C NMR spectroscopy, possess high molecular weights with broad distributions and display glass-transition temperatures (Tgs) between 7 and 96°C. The thermogravimetric analytic measurements revealed the decomposition temperature at 10% weight-loss temperatures (Td10%) ranging from 212 to 325°C. Among the hyperbranched poly(ester-amide)s obtained, the polymers with cyclohexyl molecular skeleton structure exhibit the lowest branching degree, the highest glass-transition temperatures, and the best thermal stability.
Synthesis and antimicrobial activities of N-substituted imides
Zentz, Frederic,Valla, Alain,Le Guillou, Regis,Labia, Roger,Mathot, Anne-Gabrielle,Sirot, Danielle
, p. 421 - 426 (2007/10/03)
In the field of our research programs concerning novel antimicrobial agents, a series of N-substituted imides was synthesized. These compounds were obtained by cyclization of amido-acids in acetic anhydride/sodium acetate or hexamethyldisilazane/zinc bromide for the hydroxy-aromatic derivatives. The hydroxy-alkyl maleimides were directly prepared by condensation of the corresponding amino-alcohol with maleic anhydride in boiling toluene. Most of N-substituted maleimides showed an interesting antimicrobial activity towards bacteria from the ATCC collection (Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) but the MIC values for P. aeruginosa were always high (128 μg/ml). The imides with alkyl substituents showed higher activities than aromatic analogues with MIC values in the range of 8-32 μg/ml. Comparatively, succinimides were practically inactive.
Antiherpes peptide derivatives having a 1,4-dioxo-C, N-terminus
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, (2008/06/13)
Described herein are peptide derivatives of the formula R1 NH--CO--Q--C(O)--NR2 --CH[CH2 C(O)--Y]--C(O)--NH--CH[CR3 (R4)--COOH]--C(W)--NH--CHR5 --Z wherein R1 is an optionally su
Antiherpes peptide derivatives having a 1,4-dioxo-C4 N-terminus
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, (2008/06/13)
Disclosed herein are peptide derivatives of the formula R1NH-CO-Q-C(O)-NR2-CH[CH2C(O)-Y]-C(O)-NH-CH[CR3(R4)-COOH]-C(W)-NH-CHR5-Z wherein R1 is an optionally substituted alkyl or optionally substituted phenylalkyl, R2 is hy