38053-20-2Relevant academic research and scientific papers
Non-peptide-based new class of platelet aggregation inhibitors: Design, synthesis, bioevaluation, SAR, and in silico studies
Jaiswal, Pradeep K.,Sharma, Vashundhra,Kumar, Surendra,Mathur, Manas,Swami, Ajit K.,Yadav, Dharmendra K.,Chaudhary, Sandeep
, (2018/03/21)
A series of 2-oxo-2-phenylethylidene linked 2-oxo-benzo[1,4]oxazine analogues 17a–x and 18a–o, incorporated with a variety of electron-withdrawing as well as electron-donating groups at ring A and ring C, were synthesized under greener conditions in excel
Switchable highly regioselective synthesis of 3,4-dihydro-quinoxalin-2(1H)ones from o-phenylenediamines and aroylpyruvates
Dobia?, Juraj,Ondru?, Marek,Addovà, Gabriela,Bohà?, Andrej
supporting information, p. 1350 - 1360 (2017/07/28)
3-Acylmethylidene-3,4-dihydroquinoxalin-2(1H)-ones are compounds which possess a wide range of physical and pharmaceutical applications. These compounds can be easily prepared by cyclocondensation of o-phenylenediamines and aroylpyruvates. Unsymmetrically
Furan-2,3-diones as masked dipoles: synthesis of isotetronic acids and mechanistic considerations
Barbier, Vincent,Couty, Fran?ois,David, Olivier R.P.
, p. 5646 - 5651 (2016/08/17)
The formal dipolar behaviour of furan-2,3-diones is illustrated by their reaction with ethyl glyoxylate under Lewis basic activation uniquely, giving access to isotetronic derivatives. The Janus-type nature of the activated species, both nucleophilic and
5-Aryl-1H-pyrazole-3-carboxylic acids as selective inhibitors of human carbonic anhydrases IX and XII
Cvijeti?, Ilija N.,Tan?, Muhammet,Jurani?, Ivan O.,Verbi?, Tatjana ?.,Supuran, Claudiu T.,Drakuli?, Branko J.
, p. 4649 - 4659 (2015/08/03)
Inhibitory activity of a congeneric set of 23 phenyl-substituted 5-phenyl-pyrazole-3-carboxylic acids toward human carbonic anhydrase (hCA, EC 4.2.1.1) isoforms I, II, IX and XII was evaluated by a stopped-flow CO2 hydrase assay. These compounds exerted a clear, selective inhibition of hCA IX and XII over hCAI and II, with Ki in two to one digit micromolar concentrations (4-50 μM). Derivatives bearing bulkier substituents in para-position of the phenyl ring inhibited hCA XII at one-digit micromolar concentrations, while derivatives having alkyl substituents in both ortho- and meta-positions inhibited hCA IX with Kis ranging between 5 and 25 μM. Results of docking experiments offered a rational explanation on the selectivity of these compounds toward CA IX and XII, as well as on the substitution patterns leading to best CA IX or CA XII inhibitors. By examining the active sites of these four isoforms with GRID generated molecular-interaction fields, striking differences between hCA XII and the other three isoforms were observed. The field of hydrophobic probe (DRY) appeared significantly different in CA XII active site, comparing to other three isoforms studied. To the best of our knowledge such an observation was not reported in literature so far. Considering the selectivity of these carboxylates towards membrane-associated over cytosolic CA isoforms, the title compounds could be useful for the development of isoform-specific non-sulfonamide CA inhibitors.
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors
Tumey, L. Nathan,Huck, Bayard,Gleason, Elizabeth,Wang, Jianmin,Silver, Daniel,Brunden, Kurt,Boozer, Sherry,Rundlett, Stephen,Sherf, Bruce,Murphy, Steven,Bailey, Andrew,Dent, Tom,Leventhal, Christina,Harrington, John,Bennani, Youssef L.
, p. 4915 - 4918 (2007/10/03)
Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibi
