39221-42-6Relevant articles and documents
The effect of the structure of derivatives of nitrogen-containing heterocycles on their anti-influenza activity
Gridina, Tatyana L.,Fedchuk, Alla S.,Basok, Stephan S.,Artemenko, Anatoliy G.,Ognichenko, Liudmila N.,Shitikova, Larisa I.,Lutsyuk, Anatolii F.,Gruzevskii, Aleksandr A.,Kuz’min, Victor E.
, p. 455 - 462 (2019/06/20)
[Figure not available: see fulltext.] An adequate QSAR model based on the simplex representation of the molecular structure was built in order to optimize the search for new anti-influenza agents. Structural interpretation of the model allowed us to identify molecular fragments that determine the activity of compounds against human influenza viruses. Further virtual screening and targeted synthesis allowed us to select a group of potentially effective compounds, three of which, derivatives of piperidine and isoindoline, turned out to be the most promising.
Synthesis and in Vivo Evaluation of [123I]Melanin-Targeted Agents
Roberts, Maxine P.,Nguyen, Vu,Ashford, Mark E.,Berghofer, Paula,Wyatt, Naomi A.,Krause-Heuer, Anwen M.,Pham, Tien Q.,Taylor, Stephen R.,Hogan, Leena,Jiang, Cathy D.,Fraser, Benjamin H.,Lengkeek, Nigel A.,Matesic, Lidia,Gregoire, Marie-Claude,Denoyer, Delphine,Hicks, Rodney J.,Katsifis, Andrew,Greguric, Ivan
supporting information, p. 6214 - 6224 (2015/08/24)
This study reports the synthesis, [123I]radiolabeling, and biological profile of a new series of iodinated compounds for potential translation to the corresponding [131I]radiolabeled compounds for radionuclide therapy of melanoma. Ra
Synthesis and radiosynthesis of a novel PET fluorobenzyl piperazine for melanoma tumour imaging; [18F]MEL054
Taylor, Stephen R.,Roberts, Maxine P.,Wyatt, Naomi A.,Pham, Tien Q.,Stark, Daniela,Bourdier, Thomas,Roselt, Peter,Katsifis, Andrew,Greguric, Ivan
, p. 491 - 499 (2013/07/19)
2-{2-[4-(4-[18F]-Fluorobenzyl)piperazin-1-yl]-2-oxoethyl}isoindolin-1-one ([18F]MEL054), is a new potent indolinone-based melanin binder designed to target melanotic tumours. [18F]MEL054 was prepared by an automated two-step radiosynthesis, comprising of
Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrin αiIbβ3
Krysko, Andrei A.,Samoylenko, Georgiy V.,Polishchuk, Pavel G.,Fonari, Marina S.,Kravtsov, Victor Ch.,Andronati, Sergei A.,Kabanova, Tatyana A.,Lipkowski, Janusz,Khristova, Tetiana M.,Kuz'Min, Victor E.,Kabanov, Vladimir M.,Krysko, Olga L.,Varnek, Alexandre A.
, p. 4646 - 4661 (2013/07/26)
A series of novel RGD mimetics containing phthalimidine fragment was designed and synthesized. Their antiaggregative activity determined by Born's method was shown to be due to inhibition of fibrinogen binding to αIIbβ3. Molecular docking of RGD mimetics to αIIbβ3 receptor showed the key interactions in this complex, and also some correlations have been observed between values of biological activity and docking scores. The single crystal X-ray data were obtained for five mimetics.
RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor
Krysko, Andrei A.,Samoylenko, Georgiy V.,Polishchuk, Pavel G.,Andronati, Sergei A.,Kabanova, Tatyana A.,Khristova, Tetiana M.,Kuz'Min, Victor E.,Kabanov, Vladimir M.,Krysko, Olga L.,Varnek, Alexandre A.,Grygorash, Ruslan Ya.
scheme or table, p. 5971 - 5974 (2011/10/09)
The novel RGD mimetics with phthalimidine central fragment were synthesized with the use of 4-piperidine-4-yl-butyric, 4-piperidine-4-yl-benzoic, 4-piperazine-4-yl-benzoic and 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acids as surrogates of Arg motif. T
A Simple One-step Synthesis of N-Substituted Isoindolin-1-ones. Diastereofacially Selective Protonation of an Intermediate Isoindolinol
Grigg, Ronald,Gunaratne, H. Q. Nimal,Sridharan, Visuvanathar
, p. 1183 - 1184 (2007/10/02)
α-Amino acids and their methyl esters, arylamines, heterocyclic amines and, less efficiently, aryl substituted aliphatic amines, react with o-phthaldialdehyde in the presence of acetic acid to give N-substituted isoindolin-1-ones in excellent yield; deute
Reactions of boroxazolidones with aromatic aldehydes. An easy route to derivatives of isoquinoline and iso-indolinone
Nefkens,Zwanenburg
, p. 6063 - 6066 (2007/10/02)
Boroxazolidones 1 derived from glycine and phenylalanine react with aromatic aldehydes to form the corresponding imines. The product 3 from 1a with o-carboxybenzaldehyde is converted into 4-hydroxyisoquinoline-3-carboxylic acid 6 by dimethyl sulfate, foll
Synthesis of the 5H-Pyrroloisoindole Ring with 1,3-Dipolar Cycloaddition Reactions
New, J. S.,Yevich, J. P.
, p. 1355 - 1360 (2007/10/02)
The 1,3-dipolar cycloaddition reaction between mesoionic oxazolines, formed from either 1,3-dihydro-2-substituted-2H-isoindole-1-carboxylic acids or 1,3-dihydro-1-oxo-α-substituted-2H-isoindole-2-acetic acids, and dimethylacetylene dicarboxylate has led t