29048-34-8Relevant academic research and scientific papers
Discovery of a series of 5-phenyl-2-furan derivatives containing 1,3-thiazole moiety as potent Escherichia coli β-glucuronidase inhibitors
Zhou, Tao-Shun,He, Lu-Lu,He, Jing,Yang, Zhi-Kun,Zhou, Zhen-Yi,Du, Ao-Qi,Yu, Jin-Biao,Li, Ya-Sheng,Wang, Si-Jia,Wei, Bin,Cui, Zi-Ning,Wang, Hong
, (2021/09/13)
Gut microbial β-glucuronidases have drawn much attention due to their role as a potential therapeutic target to alleviate some drugs or their metabolites-induced gastrointestinal toxicity. In this study, fifteen 5-phenyl-2-furan derivatives containing 1,3
Carbon–Carbon Bond Formation for the Synthesis of 5-Aryl-2-Substituted Furans Catalyzed by K3[Fe(CN)6]
Ambika,Singh, Pradeep Pratap
, (2021/10/05)
An efficient method for the carbon–carbon bond formation at C-5 position of 2-substituted furans to provide a range of π-diverse 5-aryl-2-substituted furan derivatives in 58–80% yield has been reported. The method employs several advantages such as use of catalytic amount of K3[Fe(CN)6] under mild conditions and short reaction time with high yields. Also, a variety of anilines with a variety of functional groups can be employed for the synthesis of 5-aryl-2-substituted furans. Graphic Abstract: [Figure not available: see fulltext.]
Thiazolidin-2-cyanamides derivatives as novel potent Escherichia coli β-glucuronidase inhibitors and their structure–inhibitory activity relationships
Chen, Jian-Wei,Cui, Zi-Ning,He, Min,Li, Ya-Sheng,Wang, Hong,Wang, Si-Jia,Wang, Ya-Kun,Wei, Bin,Zhang, Hua-Wei,Zhou, Tao-Shun
, p. 1736 - 1742 (2020/09/18)
Gut microbial β-glucuronidases have the ability to deconjugate glucuronides of some drugs, thus have been considered as an important drug target to alleviate the drug metabolites-induced gastrointestinal toxicity. In this study, thiazolidin-2-cyanamide de
2-furoylamide compound and preparation and application thereof
-
Paragraph 0036; 0038-0040; 0049, (2020/08/22)
The invention discloses a 2-furancarboxamide compound and a preparation method and application thereof. The 2-furancarboxamide compound is obtained by reacting a compound as shown in a formula II with9H-pyridino[3,4-b]indole in the presence of an acid-bin
Novel S-Thiazol-2-yl-furan-2-carbothioate Derivatives as Potential T3SS Inhibitors against Xanthomonas oryzae on Rice
Jiang, Shan,He, Min,Xiang, Xu-Wen,Adnan, Muhammad,Cui, Zi-Ning
, (2019/11/03)
Bacterial leaf blight (BLB) caused by Xanthomonas oryzae pv oryzae (Xoo) is considered as the most destructive disease of rice. The use of bactericides is among the most widely used traditional methods to control this destructive disease. The excessive an
Synthesis and biological evaluation of 2,5-disubstituted furan derivatives as P-glycoprotein inhibitors for Doxorubicin resistance in MCF-7/ADR cell
Li, Ya-Sheng,Zhao, Dong-Sheng,Liu, Xing-Yu,Liao, Yi-Xian,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning
, p. 546 - 556 (2018/04/17)
Multidrug resistance (MDR) is a tendency in which cells become resistant to structurally and mechanistically unrelated drugs, which is mediated by P-glycoprotein (P-gp). It is one of the noteworthy problems in cancer therapy. As one of the most important
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors
Hu, De-Kun,Zhao, Dong-Sheng,He, Min,Jin, Hong-Wei,Tang, Yong-Mei,Zhang, Lian-Hui,Song, Gao-Peng,Cui, Zi-Ning
, p. 3276 - 3280 (2018/08/22)
A series of 3,5-dimethylpyrazole derivatives containing 5-phenyl-2-furan moiety were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. Bioassay results showed that the title compounds exhibited considerable inhibitory activity agains
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors
Li, Ya-Sheng,Liu, Xing-Yu,Zhao, Dong-Sheng,Liao, Yi-Xian,Zhang, Lian-Hui,Zhang, Feng-Zhi,Song, Gao-Peng,Cui, Zi-Ning
, p. 3271 - 3275 (2018/08/22)
Tetrahydroquinoline and tetrahydroisoquinoline derivatives containing 2-phenyl-5-furan moiety were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The bioassay results showed that title compounds showed good inhibitory activity aga
Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents
Chiarelli, Laurent R.,Mori, Matteo,Barlocco, Daniela,Beretta, Giangiacomo,Gelain, Arianna,Pini, Elena,Porcino, Marianna,Mori, Giorgia,Stelitano, Giovanni,Costantino, Luca,Lapillo, Margherita,Bonanni, Davide,Poli, Giulio,Tuccinardi, Tiziano,Villa, Stefania,Meneghetti, Fiorella
, p. 754 - 763 (2018/06/26)
We report on the virtual screening, synthesis, and biological evaluation of new furan derivatives targeting Mycobacterium tuberculosis salicylate synthase (MbtI). A receptor-based virtual screening procedure was applied to screen the Enamine database, identifying two compounds, I and III, endowed with a good enzyme inhibitory activity. Considering the most active compound I as starting point for the development of novel MbtI inhibitors, we obtained new derivatives based on the furan scaffold. Among the SAR performed on this class, compound 1a emerged as the most potent MbtI inhibitor reported to date (Ki = 5.3 μM). Moreover, compound 1a showed a promising antimycobacterial activity (MIC99 = 156 μM), which is conceivably related to mycobactin biosynthesis inhibition.
Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors
Li, Ya-Sheng,Tian, Hao,Zhao, Dong-Sheng,Hu, De-Kun,Liu, Xing-Yu,Jin, Hong-Wei,Song, Gao-Peng,Cui, Zi-Ning
, p. 3632 - 3635 (2016/07/21)
A series of pyrazole and triazole derivatives containing 5-phenyl-2-furan functionality were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The bioassay results showed that title compounds exhibited considerable inhibitory activit
