77483-49-9Relevant academic research and scientific papers
2-Arylthio-5-iodo pyrimidine derivatives as non-nucleoside HBV polymerase inhibitors
Wang, Jie,Zhang, Liang,Zhao, Jianxiong,Zhang, Yu,Liu, Qingchuan,Tian, Chao,Zhang, Zhili,Liu, Junyi,Wang, Xiaowei
, p. 1573 - 1578 (2018/02/21)
In this study, a series of 2-arylthio-5-iodo pyrimidine derivatives, as non-nucleoside hepatitis B virus inhibitors, were evaluated and firstly reported as potential anti-HBV agents. To probe the mechanism of active agents, DHBV polymerase was isolated and a non-radioisotopic assay was established for measuring HBV polymerase. The biological results demonstrated that 2-arylthio-5-iodo pyrimidine derivatives targeted HBV polymerase. In addition, pharmacophore models were constructed for future optimization of lead compounds. Further study will be performed for the development of non-nucleoside anti-HBV agents.
Preparation method of 2,5,6 substituted pyrimidone derivative and application thereof in serving as anti-hepatitis virus drugs
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Paragraph 0035; 0036; 0037; 0038, (2017/07/22)
The invention discloses a novel 2,5,6 substituted pyrimidone derivative which is a compound as shown in a formula (I). The novel 2,5,6 substituted pyrimidone derivative has good anti-HBV virus activity, and details of the definitions of all radical groups are shown in the description. The invention further discloses a preparation method of the derivative, a pharmaceutical composition containing the derivative and application of the 2,5,6 substituted pyrimidone derivative and the pharmaceutical composition containing the 2,5,6 substituted pyrimidone derivative in serving as anti-HBV drugs. Please see the formula I in the description.
5-Iodo-2-arylalkylthio-6-aryl pyrimidin-4(3H)-ones as non-nucleoside anti-HBV agents
Zhang, Yu,Sun, Xuefeng,Fan, Ningning,Zhao, Jianxiong,Tu, Jing,Chen, Xiangmei,Liu, Junyi,Wang, Xiaowei
, p. 1438 - 1443 (2015/08/18)
A series of 5-iodo-2-arylalkylthio-6-aryl pyrimidin-4(3H)-ones, which can be considered as S-DABO derivatives, have been synthesized and their antiviral effect on extracellular HBV DNA was evaluated using the HepAD38 cell system. Compounds 6d1 and 6e3 exhibited more potent anti-HBV activity than lamivudine with EC50 values of 0.376 μM and 0.469 μM, respectively. In addition, inhibition of intracellular HBV DNA, pgRNA, HBeAg and HBsAg of compounds 6d1 and 6e3 was examined to initially infer the action mechanism. RT-PCR analysis of pgRNA demonstrated that these new S-DABO analogues could not interfere with HBV transcription. TRFIA analysis revealed that compounds 6d1 and 6e3 effectively reduced the secretion of HBeAg. These results demonstrated that 5-iodo-2-arylalkylthio-6-aryl pyrimidin-4(3H)-ones possess anti-HBV abilities and could be used as potential agents against HBV infection with an additional merit of low cytotoxicity.
Pd-catalyzed enantioselective aerobic oxidation of secondary alcohols: Applications to the total synthesis of alkaloids
Krishnan, Shyam,Bagdanoff, Jeffrey T.,Ebner, David C.,Ramtohul, Yeeman K.,Tambar, Uttam K.,Stoltz, Brian M.
supporting information; experimental part, p. 13745 - 13754 (2009/02/06)
Enantioselective syntheses of the alkaloids (-)-aurantioclavine, (+)-amurensinine, (-)-lobeline, and (-)- and (+)-sedamine are described. The syntheses demonstrate the effectiveness of the Pd-catalyzed asymmetric oxidation of secondary alcohols in diverse contexts and the ability of this methodology to set the absolute configuration of multiple stereocenters in a single operation. The utility of an aryne C-C insertion reaction in accessing complex polycyclic frameworks is also described.
A convergent and enantioselective synthesis of (+)-amurensinine via selective C-H and C-C bond insertion reactions
Tambar, Uttam K.,Ebner, David C.,Stoltz, Brian M.
, p. 11752 - 11753 (2007/10/03)
A convergent and enantioselective synthesis of the natural product amurensinine is described. The synthetic strategy takes advantage of mild and selective C-H and C-C bond insertion reactions, in addition to the palladium-catalyzed aerobic oxidative kinet
Efficient activation of zinc: Application of the Blaise reaction to an expedient synthesis of a statin intermediate
Shin, Hyunik,Choi, Bo Seung,Lee, Ki Kon,Choi, Hyeong-Wook,Chang, Jay Hyok,Lee, Kyu Woong,Nam, Do Hyun,Kim, No-Soo
, p. 2629 - 2632 (2007/10/03)
Efficient and practical in situ zinc activation was accomplished by treatment with catalytic amount of an organic acid. The protocol was applied successfully to the Blaise reaction of various nitriles. Noteworthy is the excellent Blaise transformation of (S)-4-chloro-3-trimethylsilyloxybutyronitrile (2b) into tert-butyl (S)-6-chloro-5-hydroxy-3-oxohexanoate (1), a key intermediate for the preparation of HMG-CoA reductase inhibitors (statins).
Asymmetric tandem reaction: Beckmann rearrangements/allylsilane cyclizations: Approach to the optically active cephalotaxine-framework
Schinzer, Dieter,Abel, Ulrich,Jones, Peter G.
, p. 632 - 634 (2007/10/03)
In connection with our studies of tandem reactions we report an asymmetric route to benzazepane frameworks via planar chiral η6-chromium arene complexes.
