123134-61-2Relevant academic research and scientific papers
In quest of small-molecules as potent non-competitive inhibitors against influenza
Malbari, Khushboo,Saha, Priyanka,Chawla-Sarkar, Mamta,Dutta, Shanta,Rai, Swita,Joshi, Mamata,Kanyalkar, Meena
, (2021/07/19)
A series of scaffolds namely aurones, 3-indolinones, 4-quinolones and cinnamic acid-piperazine hybrids, was designed, synthesized and investigated in vitro against influenza A/H1N1pdm09 virus. Designed molecules adopted different binding mode i.e., in 430-cavity of neuraminidase, unlike sialic acid and oseltamivir in molecular docking studies. All molecules reduced the viral titer and exhibited non-cytotoxicity along with cryo-protective property towards MDCK cells. Molecules (Z)-2-(3′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2f), (Z)-2-(4′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2g) and 2-(2′-Methoxy-phenyl)-1H-quinolin-4-one (3a) were the most interesting molecules identified in this research, endowed with robust potencies showing low-nanomolar EC50 values of 4.0 nM, 6.7 nM and 4.9 nM, respectively, compared to reference competitive and non-competitive inhibitors: oseltamivir (EC50 = 12.7 nM) and quercetin (EC50 = 0.56 μM), respectively. Besides, 2f, 2g and 3a exhibited good neuraminidase inhibitory activity in sub-micromolar range (IC50 = 0.52 μM, 3.5 μM, 1.3 μM respectively). Moreover, these molecules were determined as non-competitive inhibitors similar to reference non-competitive inhibitor quercetin unlike reference competitive inhibitor oseltamivir in kinetics studies.
Copper-Catalyzed Chemoselective Cyclization Reaction of 2-Isocyanoacetophenone: Synthesis of 4-Hydroxyquinoline Compounds
Yuan, Qing,Rao, Weidong,Wang, Shun-Yi,Ji, Shun-Jun
, p. 1279 - 1284 (2020/01/22)
A copper-catalyzed intramolecular cyclization reaction of 2-isocyanoacetophenone derivatives to afford 4-hydroxyquinolines chemoselectively is described. The transformation proceeds through enol tautomerism and a subsequent C-C bond formation. Compared to previous methods, this study provides a new protocol for the construction of 4-hydroxyquinoline compounds from functionalized isocyanides under mild conditions.
Synthesis and aromatase inhibitory activity of tetrahydroquinoline derivatives
Sabale, Prafulla M.,Walke, Priyanka,Solanki, Umang
, p. 265 - 270 (2019/01/21)
Aromatase, a cytochrome P450 hemo-protein which is responsible for estrogen biosynthesis, by the conversion of androgens to estrogens, has been an attractive target in the treatment of hormone-dependent breast cancer. As a result, a number of synthetic st
An efficient and rapid intramolecular aza-Michael addition of 2′-aminochalcones using ionic liquids as recyclable reaction media
Chelghoum,Bahnous,Bouraiou,Bouacida,Belfaitah
experimental part, p. 4059 - 4061 (2012/08/28)
A new, convenient, and efficient method for the intramolecular aza-Michael addition reaction of 2′-aminochalcones is developed using 1-n-butyl-3-methylimidazolium tetrafluoroborate as the solvent and catalyst. The ionic liquid is successfully regenerated and reused.
Synthesis and protein tyrosine phosphatase 1B-Inhibitory activity of chalcones
Zhao, Fei,Zhao, Qing-Jie,Zhang, Da-Zhi,Jin, Yong-Sheng,Zhang, Wei
experimental part, p. 5339 - 5342 (2012/06/30)
Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of type 2 diabetes and obesity. So far less work has been conducted in the structure-activity relationship of the PTP1B inhibitory activity of chalcones. In this work, a libr
