5692-27-3Relevant academic research and scientific papers
Synthesis of Imidazoles and Oxazoles via a Palladium-Catalyzed Decarboxylative Addition/Cyclization Reaction Sequence of Aromatic Carboxylic Acids with Functionalized Aliphatic Nitriles
Dai, Ling,Yu, Shuling,Lv, Ningning,Ye, Xuanzeng,Shao, Yinlin,Chen, Zhongyan,Chen, Jiuxi
supporting information, p. 5664 - 5668 (2021/08/01)
We herein report an efficient approach for the assembly of multiply substituted imidazoles and oxazoles in a single-step manner. These transformations are based on a decarboxylation addition and annulation of readily accessible aromatic carboxylic acids a
5-MEMBERED HETEROARYL COMPOUNDS CONTAINING A HYDROXAMATE MOIETY AND THEIR USE
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Page/Page column 68; 69; 172, (2020/07/31)
The present invention is directed to 5-membered heteroaryl compounds containing a hydroxamate moiety of Formula I, pharmaceutically acceptable salts or solvates thereof, and their use as sensitizers for chemotherapy of malignant tumors.
Nickel-Catalyzed Construction of 2,4-Disubstituted Imidazoles via C–C Coupling and C?N Condensation Cascade Reactions
Fang, Shengyang,Yu, Haihua,Yang, Xicheng,Li, Jianqi,Shao, Liming
supporting information, p. 3312 - 3317 (2019/06/13)
A convenient Ni(II)-catalyzed C?C and C?N cascade coupling reaction was developed to directly access various 2,4-disubstituted imidazoles. The reaction scope covers a variety of aryl and aliphatic substitutions, which demonstrate moderate-to-excellent yie
Design, Synthesis, and in Vitro and in Vivo Evaluation of an 18F-Labeled Sphingosine 1-Phosphate Receptor 1 (S1P1) PET Tracer
Rosenberg, Adam J.,Liu, Hui,Jin, Hongjun,Yue, Xuyi,Riley, Sean,Brown, Steven J.,Tu, Zhude
, p. 6201 - 6220 (2016/07/26)
Sphingosine 1-phosphate receptor 1 (S1P1) plays a pivotal signaling role in inflammatory response; because S1P1 modulation has been identified as a therapeutic target for various diseases, a PET tracer for S1P1 would be a useful tool. Fourteen fluorine-containing analogues of S1P ligands were synthesized and their in vitro binding potency measured; four had high potency and selectivity for S1P1 (S1P1 IC50 100-fold selectivity for S1P1 over S1P2 and S1P3). The most potent ligand, 28c (IC50 = 2.63 nM for S1P1) was 18F-labeled and evaluated in a mouse model of LPS-induced acute liver injury to determine its S1P1-binding specificity. The results from biodistribution, autoradiography, and microPET imaging showed higher [18F]28c accumulation in the liver of LPS-treated mice than controls. Increased expression of S1P1 in the LPS model was confirmed by immunohistochemical analysis (IHC). These data suggest that [18F]28c is a S1P1 PET tracer with high potential for imaging S1P1 in vivo.
Promiscuity and selectivity in covalent enzyme inhibition: A systematic study of electrophilic fragments
J?st, Christian,Nitsche, Christoph,Scholz, Therese,Roux, Lionel,Klein, Christian D.
supporting information, p. 7590 - 7599 (2014/12/11)
Covalent ligand-target interactions offer significant pharmacological advantages. However, off-target reactivity of the reactive groups, which usually have electrophilic properties, must be minimized, and the selectivity of irreversible inhibitors is a crucial requirement. We therefore performed a systematic study to determine the selectivity of several electrophilic groups that can be used as building blocks for covalently binding ligands. Six reactive groups with modulated electrophilicity were combined with 11 nonreactive moieties, resulting in a small combinatorial library of 72 fragment-like compounds. These compounds were screened against a group of 11 enzyme targets to assess their selectivity and their potential for promiscuous binding to proteins. The assay results showed a considerably lower degree of promiscuity than initially expected, even for those members of the screening collection that contain supposedly highly reactive electrophiles.
Reactions of (benzamidomethyl)triethylammonium chloride with some inorganic nucleophiles in aqueous media
Popovski, Emil,Bogdanov, Jane,Najdoski, Metodija,Hey-Hawkins, Evamarie
, p. 279 - 285 (2007/10/03)
A variety of benzamidomethyl derivatives were prepared in water under alkaline conditions (pH>9) via reaction of (benzamidomethyl)triethylammonium chloride (1) with different inorganic nucleophiles. Reaction of 1 with hydroxylamine did not give the expect
Synthesis of a new diaminodithiol bifunctional chelator for radiolabeling biomolecules with indium(III)
Sun, Yizhen,Martell, Arthur E.,Welch, Michael J.
, p. 5093 - 5103 (2007/10/03)
The synthesis of a new bifunctional ligand 1-(p- carboxybenzyl)-N,N'-bis-[1,1-dimethyl-1-(p- methoxybenzylthio)ethyl]ethylenediamine-N,N'-diacetic acid, di-t- butyl ester (1, nbi6ss) is described. It consists of a carboxybenzyl group substituted on a carb
N-ACYLATED α-AMINONITRILES AND THEIR CONVERSION INTO 5-AMINOOXAZOLE, 5(4H)-OXAZOLONE AND 4(5H)-IMIDAZOLONE DERIVATIVES
Verschave, P.,Vekemans, J.,Hoornaert, G.
, p. 2395 - 2404 (2007/10/02)
In contrast with the reaction of α-aminonitriles 1a, the corresponding N-acylated α-aminonitriles 1b-f and oxalyl chloride do not yield pyrazinone derivatives, but 5-aminooxazoles 9-11 or 4(5H)-imidazolones 12, the latter being converted in some cases int
Resonance Raman spectroscopic evidence for an intramolecular interaction involving th amide and dithioester groups of N-acyl glycine ethyl dithioesters
Storer, A. C.,Ozaki, Y.,Carey, P. R.
, p. 199 - 209 (2007/10/02)
The synthesis and resonance Raman spectra of several new N-acyl glycine etyl dithioesters RC(=O)NHCH2C(=S)SR are reported.The resonance Raman spectra of these compounds contain at least two peaks in the "C=S stretching region" between 1050 and 1200 cmsup
