37590-83-3Relevant academic research and scientific papers
Multitargeted Compounds Derived from (2,5-Dioxopyrrolidin-1-yl)(phenyl)-Acetamides as Candidates for Effective Anticonvulsant and Antinociceptive Agents
Abram, Micha?,Kamiński, Krzysztof,Kamiński, Rafa? M.,Latacz, Gniewomir,Lubelska, Annamaria,Mogilski, Szczepan,Rapacz, Anna
, p. 1996 - 2008 (2020/07/14)
We developed a focused set of original hybrid pyrrolidine-2,5-dione derivatives with potent anticonvulsant and antinociceptive properties. These hybrid compounds demonstrated broad-spectrum protective activity in a range of mouse models, such as the maximal electroshock (MES) test, the pentylenetetrazole-induced seizures (scPTZ), and the 6 Hz (32 mA) seizures. Compound 22 showed the most potent anticonvulsant activity (ED50 MES = 23.7 mg/kg, ED50 6 Hz (32 mA) = 22.4 mg/kg, ED50 scPTZ = 59.4 mg/kg). In addition, 22 revealed potent efficacy in the formalin-induced tonic pain. These in vivo activities of 22 are likely mediated by several targets and may result from the inhibition of central sodium/calcium currents and transient receptor potential vanilloid 1 (TRPV1) receptor antagonism. Finally, the lead compound 22 revealed drug-like absorption, distribution, metabolism, excretion, toxicity (ADME-Tox) properties in the in vitro assays, making it a potential candidate for further development in epilepsy and neuropathic pain indications.
Exfoliated nanosheets of a CuII coordination polymer modulate enzyme activity of α-chymotrypsin
Sarkar, Koushik,Dastidar, Parthasarathi
, p. 11297 - 11302 (2018/10/20)
A 2D coordination polymer derived from 5-azi-doisophthalic acid (AIA) and Cu(NO3)2 was designed with the aim of modulating the activity of a digestive enzyme α-chymotrypsin (ChT). The coordination polymer namely {[Cu0.5(m-AIA)0.5(H2 O)]·2 H2O}α (CP1) was successfully synthesized and fully characterized by single-crystal X-ray diffraction (SXRD). An exfoliated nanosheet (ENS) of CP1 was readily produced by overnight stirring of hand-ground CP1 crystals dispersed in DMSO. ENS(CP1) was demonstrated to be acting as an inhibitor of ChT; as much as ≡ 97 % inhibition of ChT was achieved with 100 mm of ENS(CP1) using N-succinyl-l-phenylalanine-p-nitroanilide (SPNA) as substrate. Enzyme kinetics data revealed that the inhibition of ChT followed a competitive pathway. An enzyme assay under varying ionic strength and varying concentration of free histidine revealed that the active site His-57 participated in coordination with the CuII metal center of ENS(CP1) thereby preventing the substrate (SPNA) from binding with the enzyme resulting in efficient inhibition.
Fast-acting insulin composition comprising a substituted anionic compound and a polyanionic compound
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Paragraph 0723-0726, (2016/04/19)
A composition, in the form of an aqueous solution, including insulin in hexameric form, at least one substituted anionic compound of non-saccharide structure and at least one polyanionic compound other than the substituted anionic compound.
Synthesis and characterization of novel peptido calixarene dimers
Zadmard, Reza,Hajiramezanali, Malihe
, p. 590 - 593 (2014/01/06)
Aniliniumcalix[4]arene dimers with peptide bridges to increase hydrogen bonding between amino acids and nucleic acid bases have been synthesized. Three different kinds of peptide bridges containing L-Alanine, L-Phenylalanine, and L-Tyrosine were prepared
Cyclodextrin assisted enantiomeric recognition of benzo[de]isoquinoline-1, 3-dione derived amino acids
Jursic, Branko S.,Patel, Paresh K.
, p. 919 - 926 (2007/10/03)
Spectroscopic evidence for enantiomeric recognition of properly modified amino acids through the cyclodextrin assisted formation of polymer like self-assemblies is presented. The requirements for the formation of these assemblies through aromatic π-π stac
ESI-MS in the study of the activity of α-chymotrypsin in aqueous surfactant media
De Angelis, Francesco,Di Tullio, Alessandra,Del Boccio, Piero,Reale, Samantha,Savelli, Gianfranco,Spreti, Nicoletta
, p. 3125 - 3130 (2007/10/03)
The catalytic activity of α-chymotrypsin on a model and a peptide substrate, in the supramolecular system enzyme-surfactant in water solution, has been studied by electrospray ionization mass spectrometry. Hydrolysis of N-succinyl-L-phenylalanine p-nitroanilide as the model compound, catalysed by α-chymotrypsin in the presence of monomeric cetyltributylammonium bromide, has been followed by UV and ESI-MS detection. Kinetic data, which are essentially identical independent of their determination techniques, show a twelve fold improvement of the enzyme catalytic efficiency when compared with the reaction carried out in the absence of the additive. Once validated, the ESI-MS technique was used to study the hydrolytic activity of the enzyme on a peptide substrate like substance P; it is worth emphasising that the spectrophotometric detection cannot be employed on peptides, where the chromophores are untouched by the hydrolytic process. Substance P hydrolyses in aqueous surfactant following dichotomic kinetics, which are initially rapid but then slow down as the reaction progress. The results presented in this paper are expected to extend studies on biocatalysis in aqueous surfactant media to a wide range of substrates, independent of their spectroscopic properties.
An investigation of the impact of molecular geometry upon microcapsule self-assembly
Bergeron, Raymond J.,Yao, Guo Wei,Erdos, Gregory W.,Milstein, Sam,Gao, Fenglan,Weimar, William R.,Phanstiel IV, Otto
, p. 6658 - 6665 (2007/10/02)
Bis-amide dicarboxylic acids derived from the condensation of malonic acid, 1,1- dimethylmalonic acid, 1,1-cyclopropane dicarboxylic acid, or maleic acid with L-phenylalanine, (L-Phe), are shown to supramolecularly self-assemble in aqueous solution. When
ACYLATION OF STEROID ALCOHOLS WITH 3-CARBOXYPROPANAMIDO ACIDS
Volovel'skii, L. N.,Rastrepina, I. A.,Popova, N. V.,Koryukina, V. N.,Kustova, S. P.
, p. 657 - 660 (2007/10/02)
Using N-(3-carboxypropanoyl)-β-phenyl-α-alanine as a model it has been established that when steroid alcohols are esterified with 3-carboxypropanamido acids, the carboxy group of the succinic acid residue takes part in the esterification reaction.In order
