Novel Iron Sequestering Agents:  Synthesis and Iron-Chelating Properties of Hexadentate Ligands Composed of 1-Hydroxy-2(1H)-pyrimidinone, ω-Amino Carboxylic Acid, and Tris(2-aminoethyl)amine

1997 ◽  
Vol 62 (11) ◽  
pp. 3618-3624 ◽  
Author(s):  
Junko Ohkanda ◽  
Jun Kamitani ◽  
Takeshi Tokumitsu ◽  
Yoko Hida ◽  
Takeo Konakahara ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Amino Carboxylic Acid

Synthesis, Characterization and In vitro Evaluation of N-Substituted- Sulfomoyl-Phenyl-Amino Carboxylic Acid Derivatives as Squalene Synthase Inhibitors

2019 ◽  
Vol 15 (4) ◽  
pp. 415-426
Author(s):  
Avani B. Chokshi ◽  
Mahesh T. Chhabria ◽  
Pritesh R. Desai
Keyword(s):  
Carboxylic Acid ◽  
Cell Line ◽  
Hepatic Cell ◽  
Squalene Synthase ◽  
Lipid Lowering ◽  
Assay Method ◽  
Aromatic Substituent ◽  
Hepatic Cell Line ◽  
Amino Carboxylic Acid

Background:Squalene Synthase is one of the cholesterol biosynthetic pathway enzymes, inhibition of which produces potent lipid lowering action. A variety of chemical classes have been evaluated for its inhibition to provide alternate antihyperlipidemic agents to statins.Methods:A series of N-substituted-sulfomoyl-phenyl-amino carboxylic acid derivatives were designed through pharmacophore modelling as Squalene Synthase inhibitors. We report here the synthesis, characterization and in vitro pharmacological screening of the designed molecules as Squalene synthase inhibitors. The target molecules were synthesized by a simple procedure and each molecule was characterized by IR, Mass, 1HNMR and 13CNMR spectroscopic techniques. As a primary site of action for cholesterol biosynthesis is liver, each of the molecules were first screened for in vitro cytotoxicity over human hepatic cell line (HepG2) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. The enzyme inhibition assay was performed on cell lysates prepared from HepG2 cells by Human Squalene Synthase ELISA kit, where test compounds were added in the nontoxic concentrations only.Results:Compound 5f was found to be most potent with the IC50 value of 11.91 µM. The CTC50 value for 5f on human hepatic cell line was > 1000 µM so it was considered that the compound was relatively safe and might be free of hepatotoxicity.Conclusion:From the results of our studies, it was observed that compounds with poly nuclear aromatic or hetero aromatic substituent on a side chain were more potent enzyme inhibitors and a distance of 4-5 atoms is optimum between amide nitrogen and hydroxyl group of carboxylic acid.

Adsorption of Metal Ions to Surface-Template Resins Prepared with Amphiphilic Styrene Monomers Bearing Amino Carboxylic Acid

1998 ◽  
Vol 71 (4) ◽  
pp. 789-796 ◽  
Author(s):  
Yoshifumi Koide ◽  
Keigo Tsujimoto ◽  
Hideto Shosenji ◽  
Mizuo Maeda ◽  
Makoto Takagi
Keyword(s):  
Carboxylic Acid ◽  
Metal Ions ◽  
Adsorption Of Metal Ions ◽  
Amino Carboxylic Acid

ChemInform Abstract: Unusual Lability of α-Silyloxy β-Amino Carboxylic Acid Derivatives.

ChemInform ◽  
2010 ◽  
Vol 29 (39) ◽  
pp. no-no
Author(s):  
M. N. GRECO ◽  
H. M. ZHONG ◽  
B. E. MARYANOFF
Keyword(s):  
Carboxylic Acid ◽  
Amino Carboxylic Acid

Synthesis and Properties of Two Amino Carboxylic Acid Gemini Surfactants

2020 ◽  
Vol 23 (6) ◽  
pp. 1033-1041
Author(s):  
Libo Xu ◽  
Zhirong He ◽  
Fu Han ◽  
Yawen Zhou ◽  
Baocai Xu
Keyword(s):  
Carboxylic Acid ◽  
Gemini Surfactants ◽  
Amino Carboxylic Acid

α-amino Carboxylic Acid

2012 ◽  
pp. 57-57
Author(s):  
Dieter Böning ◽  
Michael I. Lindinger ◽  
Damian M. Bailey ◽  
Istvan Berczi ◽  
Kameljit Kalsi ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Amino Carboxylic Acid

Phenolic Analogs of Amino Carboxylic-Acid Ligands for Tc-99m. 1. Synthesis and Characterization of N,N'-Ethylenebis[2-(-O-Hydroxyphenyl)Glycines] (Ehpg)

1987 ◽  
Vol 40 (10) ◽  
pp. 1695 ◽  
Author(s):  
JG Wilson
Keyword(s):  
Carboxylic Acid ◽  
Spectral Data ◽  
Dimethyl Ester ◽  
Synthesis And Characterization ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Amino Carboxylic Acid

Nine N,N'- ethylenebis [2-(o- hydroxyphenyl ) glycines ] ( ehpg ) have been prepared and characterized by conversion into their dimethyl ester dihydrochlorides. Their i.r ., 1H n.m.r. and f.a.b. mass spectral data are presented and discussed.

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