57395-47-8Relevant articles and documents
High-Yielding Water-Soluble Asymmetric Cyanine Dyes for Labeling Applications
Wolf, Natalia,Kersting, Louise,Herok, Christoph,Mihm, Cornelius,Seibel, Juergen
, p. 9751 - 9760 (2020)
A simple and efficient microwave-assisted synthesis of asymmetric pentamethine cyanine dyes with various functional groups was developed, which allows high-yielding results. The synthesized dyes are modifiable and suitable for single-molecule imaging in biological and medical sciences by application of click chemistry or classic esterification and amidation.
Leishmanicidal, antiproteolytic, and mutagenic evaluation of alkyltriazoles and alkylphosphocholines
Gontijo, Vanessa Silva,Espuri, Patrícia Ferreira,Alves, Rosemeire Brondi,De Camargos, Luiz Fernando,Dos Santos, Fábio Vieira,De Souza Judice, Wagner Alves,Marques, Marcos José,Freitas, Rossimiriam Pereira
, p. 24 - 33 (2015/06/30)
Abstract A series of 16 simple long-chain alkyltriazoles and two novel alkylphosphocholine derivatives containing an azide moiety were evaluated in vitro for their leishmanicidal activity against. Among the 18 compounds tested, the eight most active compounds against promastigote forms were selected for further evaluation against amastigote forms. These compounds were also evaluated for their cytotoxicity against murine macrophages and tested as inhibitors of cysteine protease rCPB2.8, an important target for development of antileishmanial drugs. The mutagenicity of some of these compounds was also evaluated in prokaryotic and eukaryotic cells to assess any genetic effects of the leishmanicidal candidates. The compound 4, an alkylphosphocholine derivative, was found to be the most potent against amastigote forms with an IC50 of 3.81 μM, comparable to that of pentamidine (IC50 = 6.62 μM) and amphotericin B (IC50 = 6.10 μM), two established leishmanicidal drugs. Compound 4 also exhibited the best selectivity index (SI) values of the series, demonstrating low toxicity against macrophages and a cLogP value higher than 5. Among the alkyltriazoles, compounds 13 and 14 were the most active against promastigote and amastigote forms. They were then evaluated for their mutagenicity in vitro; the mutagenicity index (MI) values were lower than 2, suggesting that these compounds are not mutagenic.
The design and synthesis of a 5-HETE affinity chromatography ligand for 5-hydroxyeicosanoid dehydrogenase
Khanapure, Subhash P.,Saha, Goutam,Powell, William S.,Rokach, Joshua
, p. 5807 - 5811 (2007/10/03)
The first total synthesis of an ω-amino 5-HETE derivative 27 has been accomplished by a new counter-clockwise strategy, in which C-1 is constructed first and C-20 last. The ω-amino 5-HETE derivative was transformed to an affinity chromatography ligand, the biotinylated 5-HETE 30. This affinity chromatography ligand is aimed at purifying the 5-hydroxyeicosanoid dehydrogenase enzyme, which is responsible for the conversion of 5-HETE to 5- oxo-ETE, a potent eosinophil chemotactic factor. (C) 2000 Elsevier Science Ltd.
