13246-52-1Relevant articles and documents
Synthesis of Highly Functionalized Cyclobutene Derivatives
Yavari, Issa,Bayat, Mohammad
, p. 1221 - 1227 (2003)
Protonation of the reactive 1:1 intermediates produced in the reaction between triphenyl-phosphine and dialkyl acetylenedicarboxylates with CH-acids, such as ethyl 2,4-dioxo-hexanoate and ethyl 2,4-dioxo-5-methylhexanoate, lead to vinyltriphenylphosphonium salts, which undergo an intra-molecular Wittig reaction to produce cyclobutene derivatives in fairly high yields.
Synthesis, Nematicidal Activity, and Molecular Docking of Some New Pyrazole-5-carboxamide Derivatives
Kang, Sheng-Jie,Zhao, Wen,Tan, Cheng-Xia,Weng, Jian-Quan,Peng, Wei-Li,Liu, Xing-Hai
, p. 51 - 56 (2021/04/22)
A series of new pyrazole-5-carboxamide compounds was synthesized. All the title pyrazole-5-carboxamide compounds were confirmed by nuclear magnetic resonance and mass spectrometry. The primarily nematicidal bioassay results showed that some of them exhibit low activity against Meloidogyne incognita at 10 ppm. In addition, the molecular docking simulation results indicated that compound 6b interacts with succinate dehydrogenase through two hydrogen bonds, which may provide useful information for further design novel nematicides.
CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF
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Paragraph 0518, (2018/04/17)
Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2
Ortiz Zacarías, Natalia V.,Van Veldhoven, Jacobus P. D.,Portner, Laura,Van Spronsen, Eric,Ullo, Salviana,Veenhuizen, Margo,Van Der Velden, Wijnand J. C.,Zweemer, Annelien J. M.,Kreekel, Roy M.,Oenema, Kenny,Lenselink, Eelke B.,Heitman, Laura H.,Ijzerman, Adriaan P.
, p. 9146 - 9161 (2018/10/24)
The recent crystal structures of CC chemokine receptors 2 and 9 (CCR2 and CCR9) have provided structural evidence for an allosteric, intracellular binding site. The high conservation of residues involved in this site suggests its presence in most chemokine receptors, including the close homologue CCR1. By using [3H]CCR2-RA-[R], a high-affinity, CCR2 intracellular ligand, we report an intracellular binding site in CCR1, where this radioligand also binds with high affinity. In addition, we report the synthesis and biological characterization of a series of pyrrolone derivatives for CCR1 and CCR2, which allowed us to identify several high-affinity intracellular ligands, including selective and potential multitarget antagonists. Evaluation of selected compounds in a functional [35S]GTPγS assay revealed that they act as inverse agonists in CCR1, providing a new manner of pharmacological modulation. Thus, this intracellular binding site enables the design of selective and multitarget inhibitors as a novel therapeutic approach.
