5736-94-7Relevant articles and documents
An effective dual sensor for Cu2+ and Zn2+ with long-wavelength fluorescence in aqueous media based on biphenylacrylonitrile Schiff-base
Chen, Huiling,Fang, Shuting,Guo, Hongyu,Yang, Fafu,Zha, Bowen
, (2021/12/27)
Although some sensors for Cu2+ and Zn2+ had been reported, the sensor with long-wavelength emission in aqueous media for in-situ detecting Cu2+ and Zn2+ was always expected. Herein, a biphenylacrylonitrile Schiff-base (OPBS) with large aromatic conjugated system was designed and synthesized in yield of 82%. OPBS possessed excellent long-wavelength fluorescence at 550–750 nm in aqueous media, which selectively response to sense Cu2+ with quenched fluorescence and Zn2+ with chromotropic fluorescence from red to yellow. The detection of Cu2+ and Zn2+ were realized without mutual interference in their coexistence system by means of the assistance of ATP. The detection limits were 2.3 × 10?7 M for Cu2+ and 1.8 × 10?6 M for Zn2+, respectively. The sensing mechanism was elucidated by binding MS spectra, fluorescence Job's plot and 1H NMR spectra. Moreover, OPBS exhibited good bioimaging performance and the in-situ sensing abilities for Cu2+ and Zn2+ in living cells, suggesting the application potential for detecting Cu2+ and Zn2+ in both vitro assay and vivo environment.
1,3-Oxazine-2-one derived dual-targeted molecules against replicating and non-replicating forms of Mycobacterium tuberculosis
Velappan, Anand Babu,Kesamsetty, Dhanunjaya,Datta, Dhrubajyoti,Ma, Rui,Hari, Natarajan,Franzblau, Scott G.,Debnath, Joy
supporting information, (2020/10/02)
The high mortality rate and increasing prevalence of resistant Mtb are the major concerns for the Tuberculosis (TB) treatment in this century. To curtail the prevalence of resistant Mtb, we have prepared 1,3-oxazine-2-one based dual targeted molecules. Compound 67 and 68 were found to be equally active against replicating and non-replicatiing form of Mtb (MICMABA 3.48 and 2.97 μg/ml; MICLORA 2.94 and 2.15 μg/ml respectively). They had found to suppress the biosynthesis of alfa, methoxy and keto-mycolate completely, as well as inhibit enzymatic activity of MenG (IC50 = 9.11 and 6.25 μg/ml respectively for H37Ra; IC50 = 11.76 and 10.88 μg/ml respectively for M smegmatis).
Anticancer, antimicrobial activities of quinoline based hydrazone analogues: Synthesis, characterization and molecular docking
Katariya, Kanubhai D,Shah, Shailesh R.,Reddy, Dushyanth
supporting information, (2019/11/26)
Based on the biologically active heterocycle quinoline, a series (18a-p) of quinoline hydrazone analogues were prepared, starting from 6-bromo/6-chloro-2-methyl-quinolin-4-yl-hydrazines. For all the newly synthesized compounds cytotoxic activities were carried out at the National Cancer Institute (NCI), USA, against full NCI 60 human cancer cell lines. Amongst all the tested compounds, nine compounds (18b, 18d, 18e, 18f, 18g, 18h, 18i, 18j, 18l) exhibited important anti-proliferative activity at 10 μM concentration and were further screened at 10-fold dilutions of five different concentrations (0.01, 0.1, 1, 10 and 100 μM) with GI50 values ranging from 0.33 to 4.87 μM and LC50 values ranging from 4.67 μM to >100j μM. Further, the mean values of GI50, TGI and LC50 of the most potent compound 18j were compared with the clinically used anticancer agents bendamustine and chlorambucil, revealed that the quinolyl hydrazones holds promise as a potential anticancer agents. Further all the newly prepared compounds were screened for their antimicrobial activity. All the quinolyl hydrazones displayed good to excellent antimicrobial activity with MIC values ranging from 6.25 to 100 μg/mL against the tested pathogenic strains. Molecular docking of the synthesized compounds into the active binding site of human DNA topoisomerase I (htopoI) was carried out to predict the binding mode to the DNA topoisomerase I inhibitors. Hopefully in future, compounds based on quinoline core could be used as a lead compounds for designing new anticancer agents.
