87123-08-8Relevant articles and documents
THIOL-BASED FLUORESCENT PROBE FOR REACTIVE SPECIES
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Paragraph 0168, (2020/05/29)
Detection of nitroxyl (HNO), the transient one-electron reduced form of nitric oxide, is a significant challenge owing to its high reactivity with biological thiols (rate constants as high as 109M?1 s?1). Reported herein is a new thiol-based HNO-responsive trigger that can compete against reactive thiols for HNO. This process forms an N-hydroxysulfenamide intermediate which cyclizes to release a masked fluorophore leading to fluorescence enhancement. To ensure a rapid cyclization step, the disclosed design capitalizes on two established physical organic phenomena: the alpha-effect and the Thorpe-Ingold effect. Using this new trigger, NitroxylFluor was developed; a selective HNO-responsive fluorescent probe. Treatment of NitroxylFluor with an HNO donor results in a 16-fold turn-on. This probe also exhibits excellent selectivity over various reactive nitrogen, oxygen, and sulfur species and efficacy in the presence of thiols (e.g., glutathione in mM concentrations). Also, live cell imaging of HNO using NitroxylFluor was performed.
Novel urate anion transporter 1 (URAT1) inhibitors and application thereof in medicines
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, (2017/11/04)
The invention discloses novel urate anion transporter 1 (URAT1) inhibitors and application thereof in medicines. The novel URAT1 inhibitors are compounds shown in a formula (I) and pharmacologically acceptable salts of the compounds, wherein Y or Z is respectively and independently selected from N or CH; R1 or R2 is respectively and independently selected from H, D, halogen, cyano, hydroxyl, carboxyl, C1-4 alkyl, substituted C1-4 alkyl, C3-4 cycloalkyl, C1-4 alkoxy, substituted C1-4 alkoxy, phenyl, substituted phenyl, heterocyclic aryl or substituted heterocyclic aryl; R3 or R4 is respectively and independently selected from H or C1-3 alkyl, or R3 and R4 form 3-6-membered cycloalkyl together; R5 is H, C1-4 alkyl or substituted C1-4 alkyl. The compounds provided by the invention can be applied to preparation of uric acid excretion promoting medicines, and are especially used for medicines for treating or preventing hyperuricemia or gout. The formula (I) is described in the description.
Mass Spectrometry of 2-Alkylthio-2-methylpropanoic Acids and Their Esters and Amides. Structural and Steric Effects on the McLafferty Rearrangement
Mori, Yuji,Fujiwara, Shigeru,Miyachi, Toshiko,Kitanishi, Hiroyuki,Oya, Masayuki,et al.
, p. 1505 - 1517 (2007/10/02)
The electron ionization mass spectra (MS) of S-methylated derivatives of N-(2-mercapto-2-methylpropanoyl)-L-cysteine and 2-alkylthio-2-methylpropanoic acids, as well as their esters and amides, were examined.Use of the deuterium labeling technique and accurate mass measurement supported the proposed fragmentation pathways.Extensive loss of CH2S from a molecular ion by the McLafferty rearrangementof a primary hydrogen is important in the MS of S-methyl compounds of amide derivatives.It was demonstrated that the intensity of the rearrangement ion decreases in the order of amide, ester, and acid, and in the case if amides the reaarangement is suppressed by the nonbonded interaction between methyl groups on the α carbon and the amide nitrogen.Keywords-N-(2-mercapto-2-methylpropanoyl)-L-cysteine; 2-alkylthio-2-methylpropanoic acid and methyl ester; 2-alkylthio-2-methylpropanamide; electron impact mass spectrometry; McLafferty rearrangement; steric interaction
