6332-77-0Relevant articles and documents
Dual channel selective fluorescent detection of Al3+ and PPi in mixed aqueous media: DFT studies and cell imaging applications
Alam, Rabiul,Mistri, Tarun,Bhowmick, Rahul,Katarkar, Atul,Chaudhuri, Keya,Ali, Mahammad
, p. 53940 - 53948 (2015)
A new, easily synthesizable chemosensor, DFC-EN-p-Ph-NO2, derived by the Schiff base condensation between 2,6-diformyl-p-cresol and N-(4-nitrophenyl)ethylenediamine, with potential N4O donor atoms was found to act as a dual channel (colori- and fluorimetric) sensor towards Al3+ and PPi emitting at 486 nm (blue region) and 534 nm (green region), respectively in MeOH-H2O (8 : 2, v/v) at pH 7.2 (10 mM HEPES buffer), μ = 0.05 M (LiCl), temperature 25 °C. The binding stoichiometries and formation constants of the sensor towards both Al3+ and PPi were determined by the combined UV-Vis and fluorescence titrations and Job's method, and confirmed by MS (m/z) studies. The corresponding detection limits as calculated by the 3σ method are: 7.55 μM and 3.34 μM. The most interesting part of this study is that on addition of 230 μM PPi to an ensemble of DFC-EN-p-Ph-NO2-Al3+ (20 μM Ligand and 380 μM Al3+) the fluorescence is totally quenched but on further addition of PPi a new emission peak appears at 534 nm. All biologically relevant metal ions and toxic heavy metals did not interfere with the detection of Al3+ ion. Its bio-compatibility with respect to its good solubility in mixed organo-aqueous media (MeOH-H2O) and cell permeability with no or negligible cytotoxicity provide good opportunities towards in vitro cell imaging studies of these ions. In particular, the fluorescent detection of PPi was not interfered by the presence of 400 μM of ATP or Pi although most reported PPi sensors that work in aqueous solution displayed cross-sensitivities toward ATP or Pi. The obvious excellent sensing capability of DFC-EN-p-Ph-NO2 towards PPi and Al3+ was further scrutinized in HCT116 cell lines without much cytotoxicity. The modes of 1 : 1 binding of DFC-EN-p-Ph-NO2 towards Al3+ and PPi were delineated by DFT calculations.
Synthesis, structural studies and molecular modelling of a novel imidazoline derivative with antifungal activity
Wróbel, Tomasz M.,Kosikowska, Urszula,Kaczor, Agnieszka A.,Andrzejczuk, Sylwia,Karczmarzyk, Zbigniew,Wysocki, Waldemar,Urbanczyk-Lipkowska, Zofia,Morawiak, Maja,Matosiuk, Dariusz
, p. 14761 - 14776 (2015)
Six novel imidazoline derivatives were synthesized and tested in antifungal assays. One of the compounds, N-cyclohexyl-2-imino-3-(4-nitrophenyl)imidazolidine-1-carboxamide showed moderate activity against several clinical strains of Candida albicans. Its structure was solved by X-ray crystallography and its mode of action was deduced using molecular modelling. It was found to be similar to that of fluconazole. The potential for further optimization including SAR of the compound is briefly discussed.
HETEROCYCLIC COMPOUND AS SYK INHIBITOR AND/OR SYK-HDAC DUAL INHIBITOR
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Paragraph 0175-0176, (2019/10/29)
A heterocyclic compound as a Syk inhibitor and/or a Syk-HDAC dual inhibitor, or pharmaceutically acceptable salts, prodrugs, deuterated derivatives, hydrates, and solvates thereof. Specifically, the present invention relates to a compound of formula (I), the compound having dual inhibitory activity for Syk and/or Syk-HDAC.
Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives
Lv, Kai,Li, Linhu,Wang, Bo,Liu, Mingliang,Wang, Bin,Shen, Weiyi,Guo, Huiyuan,Lu, Yu
, p. 117 - 125 (2017/06/05)
We report herein the design and synthesis of “novel imidazo [1,2-a]pyridine-3-carboxamides (IPAs)” bearing a variety of different linkers, based on the structure of IMB-1402 discovered in our lab. Results reveal that 2,6-dimethyl-N-[2-(phenylamino)ethyl] IPAs with an electron-donating group on the benzene ring as a potent scaffold. Compounds 26g and 26h have considerable activity (MIC: 0.041–2.64 μM) against drug-sensitive/resistant MTB strains, and they have acceptable safety indices against MTB H37Rv with the SI values of 4395 and 1405, respectively. Moreover, N-[2-(piperazin-1-yl)ethyl] moiety was also identified as a potentially alternative linker (compound 31), opening a new direction for further SAR studies.