A series of fifteen new compounds related to pyrazinamide (PZA) were synthesized, characterized with analytical data and screened for antimycobacterial, antifungal and antibacterial activity. The series consists of 6-chloro-5-cyanopyrazine-2-carboxamide and N-substituted 6-amino-5-cyanopyrazine-...
The preparation of novel unsymmetrical, tridentate ligand, N-methyl-N-(naphthalen-2-ylmethyl)-2-(pyridin-2-yl) ethanamine (1), has been described. Ligand 1 reacts with Pd(OAc)2 to give the corresponding cyclometallated complex, which could not be isolated. The substitution reactions of the in-si...
Through preparation and examination of a series of novel 4-amino-2-phenylpyrimidine derivatives as agonists for GPR119, we identified 2-(4-bromophenyl)-6-methyl-N-[2-(1-oxidopyridin-3-yl)ethyl]pyrimidin-4-amine (9t). Compound 9t improved glucose tolerance in mice following oral administration an...
It has been shown previously that 4-anilino quinazolines compete with the ability of ATP to bind the epidermal growth factor receptor (EGF-R), inhibit EGF-stimulated autophosphorylation of tyrosine residues in EGF-R, and block EGF-mediated growth. Since millimolar concentrations of ATP in cells ...
This work reports the synthesis of a new series of 2-aryl-6-(phenylethynyl)-4-(trifluoromethyl) quinolines (2), where aryl = 4-(phenylethynyl)phenyl (2a), Ph (2b), 4-MeC6H4 (2c), 4-FC6H4 (2d). These were obtained by the Sonogashira coupling reaction producing 42–88% yield, utilizing 6-bromoquin...
Quinoxalines are nitrogen-embedded heterocyclic compounds that possess unique and versatile pharmacological applications. The present article describes synthesis and characterization of organic salt 2-((4-bromophenyl)amino)pyrido [1,2-a]quinoxalin-11-ium bromide (BAPQ), an oxidative cyclized pro...
Experimental and theoretical investigations on the molecular structure, electronic and vibrational properties of the title compound are presented in this study. The asymmetric unit of the 2-amino-4-(3-bromophenyl)-1,3,5-triazinobenzimidazolium chloride consists of a discrete protonated cations a...
SummaryPeroxiredoxin 1 (Prx1) and glutaredoxin 3 (Grx3) are two major antioxidant proteins that play a critical role in maintaining redox homeostasis for tumor progression. Here, we identify the prototypical pyranonaphthoquinone natural product frenolicin B (FB) as a selective inhibitor of Prx1 ...
Schizothorax prenanti (Cypriniformes, Cyprinidae, Schizothoracinae) is an endemic, valuable fish in the southwest of China. Although a series of studies concerning the genetic and endocrine control of feeding and growth in S. prenanti have been examined in our laboratory, the mechanism is still ...
Mammalian target of rapamycin (mTOR) controls cellular growth and proliferation by virtue of its ability to regulate protein translation. Eukaryotic initiation factor 4E (eIF4E) binding protein 1 (4E-BP1) — a key mTOR substrate, binds and sequesters eIF4E to impede translation initiation that i...
Upon occurrence of kidney injury, tubular cells arrested in G2/M stage may promote interstitial fibroblast activation and kidney fibrosis through producing large amounts of pro-fibrotic cytokines. MTORC1 signaling is essential for controlling cell growth, however, the role and mechanisms for mTO...
AimsTo investigate the role and underlying mechanism of 4E-BP1 and S6K1 in regulating autophagy and hepatitis B virus (HBV) replication.
SummaryRecent estimates of the human proteome suggest there are ∼20,000 protein-coding genes, the protein products of which contain >145,000 phosphosites. Unfortunately, in-depth examination of the human phosphoproteome has outpaced the ability to annotate the kinases that mediate these post-tr...
The cap dependent translation initiation is a tightly controlled process of cooperative ternary complex formation by 4E-BP1, eIF4E and the 5′ cap of eukaryotic mRNA in response to environmental cues like glucose, nutrients and growth factor levels. Based on the well-described effects of mTORC1/...
The fluorinated β-diketone ligand, 4,4,4-trifluoro-1-(6-methoxy- naphthalen-2-yl)-butane-1,3-dione (HL), and its ternary europium (III) complexes using water (H2O), 2,2-dipyridine (Bipy), 1,10-phenanthroline (Phen) and 4′-phenyl-terpyridine (Phterpy) as the secondary ligand were synthesized an...
Phosphoribulokinase (PRK) is a key enzyme in the Calvin cycle of autotrophic organisms. We have constructed a spinach leaf cDNA library in the phage expression vector, λgt11, and used a rabbit polyclonal antibody raised against spinach PRK to identify PRK clones. Analyses of the nucleotide sequ...
Phosphoribulokinase from spinach is deactivated by reversible oxidation of Cys16 and Cys55 to an intrasubunit disulfide. Both residues have been assigned to the nucleotide-binding domain of the active site. Clearly, Cys16 does not play a significant role in catalysis, as complete methylation of ...
The molecule (S)-2,3-Dihydro-5,7-dihydroxy-2(3-hydroxy-4-methoxyphenyl)-4H-1-benzopyran-4-one (Hesperetin) was optimized utilizing density functional theory (DFT) with B3LYP/6-311G(d,p) basis set. The vibrational frequencies and potential energy distribution (PED)% of Hesperetin molecule was com...
In the present work 4-(1E,3Z,6E)-3-hydroxy-7-(4-hydroxy-3-methoxyphenyl)-5-oxohepta-1,3,6-trien-1-yl)-2-methoxyphenyl 4-nitrobenzoate (2), a novel curcumin ester was synthesized. The molecular structure and spectroscopic analysis were performed using experimental techniques like FT-IR, 1H,13C NM...
Curcumin (1), isolated as a major component from the chloroform extract of Curcuma longa was converted to its ester derivative 4-((1E, 6E)-7-(4-hydroxy-3-methoxyphenyl)-3,5-dioxohepta-1,6-dienyl)-2-methoxyphenyl 4-fluorobenzoate (2). The compound has been characterized with the help of 1H, 13C N...
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