874813-04-4Relevant academic research and scientific papers
INHIBITOR COMPOUNDS
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Page/Page column 63; 66, (2021/01/29)
The disclosure relates to heterocyclic compounds and methods for their preparation. The disclosure provides compounds that may have beneficial therapeutic activity in the treatment of a disease or condition mediated by excessive or otherwise undesirable Des1 and/or fibrotic activity.
Electrochemical Difunctionalization of Styrenes via Chemoselective Oxo-Azidation or Oxo-Hydroxyphthalimidation
Jiang, Haobin,Wang, Feng,Ye, Zenghui,Zhang, Fengzhi,Zhu, Rongjin
supporting information, p. 8240 - 8245 (2021/11/17)
Atom- and step-economic oxo-azidation and oxo-hydroxyphthalimidation of styrenes have been developed under mild electrolytic conditions, respectively. Various valuable alpha-azido or hydroxyphthalimide aromatic ketones were synthesized efficiently from readily available styrenes, azides, and N-hydroxyphthalimides. Mechanism studies show that two different pathways involved in these two transformations.
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents
Bangalore, Pavan K.,Vagolu, Siva K.,Bollikanda, Rakesh K.,Veeragoni, Dileep K.,Choudante, Pallavi C.,Misra, Sunil,Sriram, Dharmarajan,Sridhar, Balasubramanian,Kantevari, Srinivas
supporting information, p. 26 - 35 (2020/01/03)
(+)-Usnic acid, a product of secondary metabolism in lichens, has displayed a broad range of biological properties such as antitumor, antimicrobial, antiviral, anti-inflammatory, and insecticidal activities. Interested by these pharmacological activities and to tap into its potential, we herein present the synthesis and biological evaluation of new usnic acid enaminone-conjugated 1,2,3-triazoles 10-44 as antimycobacterial agents. (+)-Usnic acid was condensed with propargyl amine to give usnic acid enaminone 8 with a terminal ethynyl moiety. It was further reacted with various azides A1-A35 under copper catalysis to give triazoles 10-44 in good yields. Among the synthesized compounds, saccharin derivative 36 proved to be the most active analogue, inhibiting Mycobacterium tuberculosis (Mtb) at an MIC value of 2.5 μM. Analogues 16 and 27, with 3,4-difluorophenacyl and 2-acylnaphthalene units, respectively, inhibited Mtb at MIC values of 5.4 and 5.3 μM, respectively. Among the tested Gram-positive and Gram-negative bacteria, the new derivatives were active on Bacillus subtilis, with compounds 18 [3-(trifluoromethyl)phenacyl] and 29 (N-acylmorpholinyl) showing inhibitory concentrations of 41 and 90.7 μM, respectively, while they were inactive on the other tested bacterial strains. Overall, the study presented here is useful for converting natural (+)-usnic acid into antitubercular and antibacterial agents via incorporation of enaminone and 1,2,3-triazole functionalities.
Visible-light-enabled oxyazidation of alkenes leading to α-azidoketones in air
Wei, Wei,Cui, Huanhuan,Yue, Huilan,Yang, Daoshan
supporting information, p. 3197 - 3202 (2018/07/29)
A new and facile visible-light-enabled method for the synthesis of α-azidoketones has been developed via oxyazidation of alkenes with TMSN3 in air at room temperature. A series of α-azidoketones could be easily and efficiently obtained in moder
Method for preparing alpha-azidoketone compounds based on photocatalysis
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Paragraph 0162; 0163; 0164, (2018/10/11)
The invention discloses a method for preparing alpha-azidoketone compounds based on photocatalysis. The method is based on a reaction formula shown in the description, wherein R is optionally-substituted aryl, heteroaryl or 1-12 carbon alkyl; R is o
Catalytic asymmetric hydrogenation of N-Boc-imidazoles and oxazoles
Kuwano, Ryoichi,Kameyama, Nao,Ikeda, Ryuhei
supporting information; experimental part, p. 7312 - 7315 (2011/06/24)
Substituted imidazoles and oxazoles were respectively hydrogenated into the corresponding chiral imidazolines and oxazolines (up to 99% ee). The highly enantioselective hydrogenation was achieved by using the chiral ruthenium catalyst, which is generated
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
Perner, Richard J.,Koenig, John R.,Didomenico, Stanley,Gomtsyan, Arthur,Schmidt, Robert G.,Lee, Chih-Hung,Hsu, Margaret C.,McDonald, Heath A.,Gauvin, Donna M.,Joshi, Shailen,Turner, Teresa M.,Reilly, Regina M.,Kym, Philip R.,Kort, Michael E.
supporting information; experimental part, p. 4821 - 4829 (2010/08/06)
The synthesis and structure-activity relationships of a series of 5-monosubstituted and 4,5-disubstituted 2-arylaminooxazoles as novel antagonists of the transient receptor potential vanilloid 1 (TRPV1) receptor are described. The 7-hydroxy group of the t
11-Beta HSD1 inhibitors
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Page/Page column 32, (2008/06/13)
This invention relates to inhibiting 11-beta HSD1.
