79498-51-4Relevant academic research and scientific papers
In Silico Discovery and Validation of Amide Based Small Molecule Targeting the Enzymatic Site of Shiga Toxin
Chauhan, Vinita,Chaudhary, Dilip,Pathak, Uma,Saxena, Nandita,Dhaked, Ram Kumar
, p. 10763 - 10773 (2016)
Shiga toxin (Stx), a category B biothreat agent, is a ribosome inactivating protein and toxic to human and animals. Here, we designed and synthesized small molecules that block the active site of the Stx A subunit. On the basis of binding energy, 20 molec
Mild, rapid and efficient metal-free synthesis of 2-aryl-4-aryloxyquinolines via direct Csp2[sbnd]O bond formation by using diaryliodonium salts
Nahide, Pradip D.,Solorio-Alvarado, César R.
supporting information, p. 279 - 284 (2017/01/03)
An efficient ligand- and transition metal-free procedure for the direct Csp2[sbnd]O bond formation for the arylation of 2-aryl-4-quinolones was developed. The synthesis of the starting quinolones was carried out under our optimized C
Selective Oxidative Decarbonylative Cleavage of Unstrained C(sp3)-C(sp2) Bond: Synthesis of Substituted Benzoxazinones
Verma, Ajay,Kumar, Sangit
supporting information, p. 4388 - 4391 (2016/10/11)
A transition metal (TM)-free practical synthesis of biologically relevant benzoxazinones has been established via a selective oxidative decarbonylative cleavage of an unstrained C(sp3)-C(sp2) bond employing iodine, sodium bicarbonate, and tbutyl hydroperoxide in DMSO at 95 °C. Control experiments and Density Functional Theory (DFT) calculations suggest that the reaction involves a [1,5]H shift and extrusion of CO gas as the key steps. The extrusion of CO has also been established using PMA-PdCl2.
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and v
Marques, Emerson F.,Bueno, Mauro A.,Duarte, Patricia D.,Silva, Larissa R.S.P.,Martinelli, Ariani M.,Dos Santos, Caio Y.,Severino, Richele P.,Broemme, Dieter,Vieira, Paulo C.,Correa, Arlene G.
experimental part, p. 10 - 21 (2012/08/28)
Cathepsins, also known as lysosomal cysteine peptidases, are members of the papain-like peptidase family, involved in different physiological processes. In addition, cathepsins are implicated in many pathological conditions. This report describes the synthesis and evaluation of a series of N-arylanthranilic acids, acridones, and 4-quinolinones as inhibitors of cathepsins V and L. The kinetics revealed that compounds of the classes of acridones are reversible competitive inhibitors of the target enzyme with affinities in the low micromolar range. They represent promising lead candidates for the discovery of novel competitive cathepsin inhibitors with enhanced selectivity and potency. On the other hand, 4-quinolinones were noncompetitive inhibitors and N-arylanthranilic acids were uncompetitive inhibitors.
HETEROCYCLIC AND BICYCLIC COMPOUNDS, COMPOSITIONS AND METHODS
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Page/Page column 127, (2010/11/08)
The present invention provides, among other things, new bicyclo heterocyclic compounds, compositions comprising these heterocyclic compounds, methods of making the heterocyclic compounds, and methods of using these heterocyclic compounds for treating a variety of conditions and disease states associated with, for example, cellular proliferation, inflammation, glycosidase expression, or the low expression of Perlecan.
Tautomeric 2-arylquinolin-4(1H)-one derivatives- spectroscopic, X-ray and quantum chemical structural studies
Mphahlele, Malose J.,El-Nahas, Ahmed M.
, p. 129 - 136 (2007/10/03)
A convenient method for the synthesis of 2-aryl-1-methylquinolin-4(1H) -ones is described. Spectroscopic and X-ray crystallographic techniques as well as quantum chemical calculations have been used to probe the structure of potentially tautomeric 2-arylq
THE REARRANGEMENT OF HYDROPEROXYINDOLENINES
McCapra, F.,Long, P. V.
, p. 3009 - 3012 (2007/10/02)
Examination of a series of substituted 3-(hydroxyperoxy)indolenines favours a mechanism for base catalysed decomposition of the dioxetan rather than Criegee type.
