3718-21-6Relevant articles and documents
Thermal [3 + 2] cycloaddition of N-iminoquiazoline ylides with allenoates for synthesis of tetrahydropyrazoloquinazoline derivatives
Zhang, Xu,Yuan, Chunhao,Zhang, Cheng,Gao, Xing,Wang, Bo,Sun, Zhanhu,Xiao, Yumei,Guo, Hongchao
, p. 8274 - 8281 (2016)
The thermal [3 + 2] cycloaddition reaction of N-iminoquiazoline ylides with allenoates worked efficiently under mild reaction conditions to provide a variety of tetrahydropyrazoloquinazoline derivatives in good to excellent yields and moderate to excellen
Synthesis, in-vitro and in-silico studies of triazinoindole bearing bis-Schiff base as β-glucuronidase inhibitors
Ahmad, Shakeel,Aziz, Aamir,Khan, Fahad,Rahim, Fazal,Sarfraz, Maliha,Taha, Muhammad,Ullah, Hayat,Wadood, Abdul
, (2021/07/16)
Triazinoindole bearing bis-Schiff base analogs (1–20) were synthesized by triazinoindole-thione ring formation, triazinoindole-thiol-phenylethanone, followed by triazinoindole bis-Schiff base formation. Synthesized analogs showed β-glucuronidase potential with IC50 value ranging between 2.60 ± 0.10 to 55.40 ± 1.60 μM as compared to standard D-saccharic acid 1,4-lactone (IC50 = 48.10 ± 1.2 μM). Analog 20 was the most potent one with IC50 value 2.60 ± 0.10 μM. Analogs 17, 4 showed IC50 values 5.20 ± 0.20 and 5.70 ± 0.20 μM respectively and withstand 2nd and 3rd ranked scaffolds among the synthesized analogs. All other sixteen analogs showed many-fold better potency with IC50 values ranging from 7.9 ± 0.2 to 48.1 ± 1.2 μM. The structure-activity relationship was established and confirmed of binding interactions through molecular docking studies.
Denitrogenative Hydrotrifluoromethylation of Benzaldehyde Hydrazones: Synthesis of (2,2,2-Trifluoroethyl)arenes
Zhao, Zhensheng,Ma, Kevin C. Y.,Legault, Claude Y.,Murphy, Graham K.
supporting information, p. 11240 - 11245 (2019/08/20)
Reacting hydrazones of arylaldehydes with Togni's CF3-benziodoxolone reagent, in the presence of potassium hydroxide and cesium fluoride, induces a denitrogenative hydrotrifluoromethylation event to produce (2,2,2-trifluoroethyl)arenes. This novel reaction was tolerant to many electronically-diverse functional groups and substitution patterns, as well as naphthyl- and heteroaryl-derived substrates. Advantages of this process include the easy access to hydrazone precursors on a large scale, speed and operational simplicity, and being transition metal-free.
Colorimetric anion sensors based on positional effect of nitro group for recognition of biologically relevant anions in organic and aqueous medium, insight real-life application and DFT studies
Singh, Archana,Sahoo, Suban K.,Trivedi, Darshak R.
, p. 596 - 610 (2017/08/07)
A new six colorimetric receptors A1-A6 were designed and synthesized, characterized by typical common spectroscopic techniques like FT-IR, UV–Visible, 1H NMR, 13C NMR and ESI-MS. The receptor A1 and A2 exhibit a significant naked-eye response towards F? and AcO? ions in DMSO. Due to presences of the NO2 group at para and ortho position with extended π-conjugation of naphthyl group carrying –OH as a binding site. Compared to receptor A2, A1 is extremely capable of detecting F? and AcO? ions present in the form of sodium salts in an aqueous medium. This is owed to the occurrence of –NO2 group at para position induced in increasing the acidity of –OH proton. Consequently, it easily gets deprotonated in aqueous media. The detection limit of receptor A1 was turned out to be 0.40 and 0.35?ppm for F? and AcO? ions which is beneath WHO permission level (1.0?ppm). Receptor A1 shows a solitary property of solvatochromism in different aprotic solvents in presence of AcO? ion. Receptor A1 depicts high selectivity towards AcO? ion in DMSO: HEPES buffer (9:1, v/v). Receptor A1 proved itself for real life application by detecting anion in solution and solid state. The binding mechanism of receptor A1 with AcO? and F? ions was monitored from 1HNMR titration and DFT study.
