72000-24-9Relevant academic research and scientific papers
Identification of a Novel Oxadiazole Inhibitor of Mammalian Target of Rapamycin
Lim, Sunwoo,Lee, Hyomin,Kim, Euijung,Hur, Wooyoung
, p. 296 - 303 (2020/02/04)
We performed a biochemical screen against mTOR using in-house small molecule library. Two novel, structurally distinct hits were identified. Among them, a novel oxadiazole scaffold compound (2) suppressed the phosphorylation of both S6K1 and Akt1 in HeLa cells. Docking study suggested that 2 is ATP-competitive and shows a pi-pi interaction with Trp2239 and hydrogen bonds with Trp2239 and Thr2245. Through derivatization, a slightly more potent analogue (2a) was identified with IC50 of 9.6 μM. Our study provides a starting point for discovery of novel potent mTOR inhibitors.
Deep eutectic solvents as convenient media for synthesis of novel coumarinyl schiff bases and their QSAR studies
Molnar, Maja,Komar, Mario,Brahmbhatt, Harshad,Babi?, Jurislav,Joki?, Stela,Rastija, Vesna
, (2017/09/25)
Deep eutectic solvents, as green and environmentally friendly media, were utilized in the synthesis of novel coumarinyl Schiff bases. Novel derivatives were synthesized from 2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)acetohydrazide and corresponding aldehyde
Synthesis and characterization of new thiazolidinones containing coumarin moieties and their antibacterial and antioxidant activities
Hamdi, Naceur,Al-Ayed, Abdullah Sulaiman,Said, Ridha Ben,Fabienne, Alary
, p. 9321 - 9334 (2012/11/07)
New coumarin derivatives namely (2-(4-methyl-2-oxo-2H-chromen-7-yloxy)- N-(4-oxo-2-phenylthiazolidin-3-yl)acetamide, N-(2-(3-methoxyphenyl)-4- oxothiazolidin- 3-yl)-2-(4-methyl-2-oxo-2H-chromen-7-yloxy)acetamide, 2-(4-methyl-2-oxo-2H-chromen- 7-yloxy)-N-(
Synthesis and spectrophotometric determination of 7-hydroxy-4-methyl coumarin containing schiff base derivatives with potential antimicrobial and antioxidant activities
Satyanarayana,Rakshit, Madhumita,Sivakumar
, p. 1295 - 1301 (2012/01/02)
2-[(4-Methyl-2-oxo-2H-chromen-7-yl)oxy]acetohydrazide (3), aryl/hetero aromatic aldehydes were condensed under reflux temperature for the synthesis of new Schiff base 2-[(4-methyl-2-oxo-2H-chromen-7-yl)oxy]-N'- (substitutedmethylene)acetohydrazides (4a-l)
Synthesis and antimicrobial activity of thiazolidinones derived from 4-methylcoumarinyl-7-oxyacetic hydrazide
Manojkumar,Ravi,Gopalakrishnan
experimental part, p. 954 - 958 (2010/08/05)
A series of new thiazolidin-4-ones (3a-j), 5-carboxymethyl-4- thiazolidinones (4a-1) have been synthesised via the condensation of 4-methylcoumarinyl-7-oxyacetic acid [(substituted phenyl)methylene]hydrazides (2a-1), with thioglycolic acid and thiomalic acid respectively. The compounds (2a-1) were synthesised from 4-methylcoumarinyl-7-oxyacetic hydrazide using various aromatic aldehydes. The structure of all synthesised compounds has been determined by spectral methods. The compounds were screened for their antibacterial activity against S. aureus and B. subtilis bacteria.
