33840-90-3Relevant academic research and scientific papers
A high signal-to-background ratio H2S-specific fluorescent probe based on nucleophilic substitution and its bioimaging for generation H2S induced by Ca2+ in vivo
Kang, Jin,Huo, Fangjun,Yao, Yishan,Yin, Caixia
, (2019)
Hydrogen sulfide (H2S), a new endothelium-derived relaxing factor (EDRF), which plays vital roles in regulating intracellular redoxstatus and other fundamental signaling processes involved in human health and disease. In this work, we designed a fluorescent probe for H2S successive nucleophilic reaction with high signal-to-background (S/B) ratio. In the probe, we utilized 2-mercaptobenzoic acid as the distinguish reaction site and introduced 2,4-dinitrophenyl to provide appropriate steric hindrance to realize specific response on well-structured H2S. Other substances sulfur-containing do not disturb the detection of H2S. The max emission with 197-fold enhancement exhibits high signal-to-background ratio. The detection limit was calculated to be 64 nM. Imaging assays in living cells showed that the probe could penetrate cells membrane easily and allowed to detect endogenous generation H2S induced by Ca2+ mediated cystathionine γ-lyase (CSE). Moreover, the probe was successfully used to detect exogenous H2S in mice.
Sulfur Oxidation Increases the Rate of HIRE-Type [1.4]Thiazepinone Ring Expansion and Influences the Conformation of a Medium-Sized Heterocyclic Scaffold
Reutskaya, Elena,Sapegin, Alexander,Peintner, Stefan,Erdélyi, Máté,Krasavin, Mikhail
, p. 5778 - 5791 (2021/05/07)
The hydrated imidazoline ring expansion (HIRE-type) reaction was investigated for a series of di(hetero)arene-fused [1.4]thiazepinones in comparison with their sulfone counterparts. The sulfones were found to undergo ring expansion at a much higher rate compared to the thioethers, much in line with the current mechanistic understanding of the process. Moreover, the amide bond cis- and trans-isomers of the ring-expanded products were found, in the case of sulfones, to be stabilized through an intramolecular hydrogen bond. The latter phenomenon was studied in detail by NMR experiments and corroborated by X-ray crystallographic information.
Benzothiazole-based hydrogen sulfide fluorescent probe as well as preparation method and application thereof
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Paragraph 0023-0025, (2020/10/30)
The invention discloses a benzothiazole-based hydrogen sulfide fluorescent probe as well as a preparation method and application thereof. The structural general formula of the fluorescent probe compound is shown as a formula (I). The compound is simple to synthesize, the fluorescence of the compound is remarkably enhanced after the compound reacts with hydrogen sulfide, and the compound shows goodselectivity on hydrogen sulfide, shows a very good linear relationship within a certain concentration range, and can be used as a fluorescent probe for qualitative and quantitative detection of hydrogen sulfide. In addition, raw materials for preparing the compound are cheap and easily available, the cost is low, the preparation process is simple, and the probe is suitable for large-scale industrial popularization and application.
SELECTIVE BROMODOMAIN INHIBITION OF FUNGAL BDF1
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Page/Page column 43-44, (2018/02/28)
The invention provides antifungal compounds, antifungal compositions, and intermediates for the preparation of antifungal compounds and antifungal compositions. The invention also provides methods of inhibiting fungi and methods of treating fungal infecti
Denitrocyclization in synthesis of dibenzo[b,f][1,4]thiazepin-11(10H)-ones and their derivatives
Smirnov, Alexey V.,Kalandadze, Levari S.,Sakharov, Vladimir N.,Dorogov, Mikhail V.,Ivachtchenko, Alexander V.
, p. 1247 - 1251 (2008/09/18)
(Chemical Equation Presented) A convenient synthesis of the novel dibenzo[b,f][1,4]thiazepin-11(10H)-ones is reported. As a key step, the synthetic route includes intramolecular aromatic denitrocyclization of 2-(2,4-dinitro-phenylsulfanyl)-benzoic acid am
Denitrocyclisation in the synthesis of dibenzothiazepinones
Smirnov, Alexey V.,Kalandadze, Levan S.,Sakharov, Vladimir N.,Dorogov, Mikhail V.
, p. 262 - 264 (2007/10/03)
A new method has been elaborated for the synthesis of new compounds of the dibenzothiazepine series by intramolecular aromatic substitution of the nitro group.
Fluorinated diaryl sulfides as serotonin transporter ligands: Synthesis, structure-activity relationship study, and in vivo evaluation of fluorine-18-labeled compounds as PET imaging agents
Huang, Yiyun,Bae, Sung-A,Zhu, Zhihong,Guo, Ningning,Roth, Bryan L.,Laruelle, Marc
, p. 2559 - 2570 (2007/10/03)
A series of new, fluorine-containing substituted diphenyl sulfides was synthesized to serve as candidate ligands for positron emission tomography (PET) imaging of the serotonin transporter (SERT) and to further probe the structure-activity relationship (S
