5798-75-4Relevant articles and documents
Combination of a new chiroptical probe and theoretical calculations for chirality detection of primary amines
Kuwahara, Shunsuke,Nakamura, Masaya,Yamaguchi, Akira,Ikeda, Mari,Habata, Yoichi
, p. 5738 - 5741 (2013)
A method to determine absolute configurations of primary amines by combined use of a chiroptical probe 1 and theoretical calculations is reported. Probe 1 is linked to chiral primary amines yielding 1-amine conjugates, which exhibited exciton coupled circular dichroism in the m-quaterphenyl chromophores. The ratios between the P and M conformers of the 1-amine conjugates, which are calculated with DFT, were correlated highly with the sign and amplitude of the observed CD spectra.
Novel cycloaddition of 2-alkyl-3-benzoyl-2-thianaphthalenes
Shimizu, Hiroshi,Yonezawa, Takenori,Watanabe, Tomoko,Kobayashi, Kazuhiro
, p. 1659 - 1660 (1996)
Deprotonation of 2-alkyl-3-benzoyl-2-thiochromenium salts 1 or 2 with 2 equiv. of triethylamine in ethanol affords the unexpected benzothiopyran derivatives 3 and 4; the structure of 3a is confirmed by X-ray crystallography.
Schiff Base Functionalized 1,2,4-Triazole and Pyrene Derivative for Selective and Sensitive Detection of Cu2+?ion?in the Mixed Organic- Aqueous Media
Choi, Nam Gyu,Vanjare, Balasaheb D.,Mahajan, Prasad G.,Nagarajan, Rajendran,Ryoo, Hyang Im,Lee, Ki Hwan
, p. 1739 - 1749 (2021/09/03)
We have prepared Schiff base functionalized 1,2,4-triazole and pyrene derivative for selective, sensitive, and naked eye colorimetric detection of Cu2+ in the mixed organic- aqueous media. Amongst the 18 different metal ions studied for absorption and fluorescence titration, only Cu2+ ion encourages the modification in spectral properties of Schiff base functionalized 1,2,4-Triazole and Pyrene Probe. The stoichiometric ratio of the TP-Cu2+ complex was determined to be 2:1 according to Job’s plot. The lower detection limit estimated for Cu2+ is 0.234?nM which shows excellent sensitivity and selectivity of the present analytical method towards detection of Cu2+ ion in the mixed organic-aqueous media. The present approach has been successfully utilized for the quantitative determination of Cu2+ ion from environmental aqueous solution.
Synthesis and biological evaluation of honokiol derivatives bearing 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3h)-ones as potential viral entry inhibitors against sars-cov-2
Bai, Li-Ping,Guo, Yong,Jiang, Zhi-Hong,Liu, Jia-Zheng,Meng, Jie-Ru,Xu, Ting,Zheng, Zhi-Yuan
, (2021/09/08)
The 2019 coronavirus disease (COVID-19) caused by SARS-CoV-2 virus infection has posed a serious danger to global health and the economy. However, SARS-CoV-2 medications that are specific and effective are still being developed. Honokiol is a bioactive component from Magnoliae officinalis Cortex with damp-drying effect. To develop new potent antiviral molecules, a series of novel honokiol analogues were synthesized by introducing various 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3H)-ones to its molecule. In a SARS-CoV-2 pseudovirus model, all honokiol derivatives were examined for their antiviral entry activities. As a result, 6a and 6p demonstrated antiviral entry effect with IC50 values of 29.23 and 9.82 μM, respectively. However, the parental honokiol had a very weak antiviral activity with an IC50 value more than 50 μM. A biolayer interfero-metry (BLI) binding assay and molecular docking study revealed that 6p binds to human ACE2 protein with higher binding affinity and lower binding energy than the parental honokiol. A competitive ELISA assay confirmed the inhibitory effect of 6p on SARS-CoV-2 spike RBD’s binding with ACE2. Importantly, 6a and 6p (TC50 > 100 μM) also had higher biological safety for host cells than honokiol (TC50 of 48.23 μM). This research may contribute to the discovery of potential viral entrance inhibitors for the SARS-CoV-2 virus, although 6p’s antiviral efficacy needs to be validated on SARS-CoV-2 viral strains in a biosafety level 3 facility.
