71149-97-8Relevant academic research and scientific papers
Synthesis of novel pyridazine derivatives as potential antimicrobial agents
Behalo, Mohamed S.,Gad El-Karim, Iman A.,Issac, Yvette A.,Farag, Mohamed A.
, p. 661 - 673 (2014)
A series of novel pyridazine derivatives incorporated with triazole, thiazolidine, imidazolidine, oxazine, and quinazoline moieties was synthesized by the reaction of [6-(4-phenoxyphenyl)pyridazin-3-yloxy]acetyl isothiocyanate with variety of nucleophilic
COMPOUNDS AND METHODS OF THEIR USE
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Page/Page column 87, (2020/05/19)
Provided are agents capable of binding the KIX domain of CBP or MED15 to inhibit the binding between SREBP1 and the KIX domain of MED15 or CBP. Also provided are compositions containing the agents and methods of their use.
Design, synthesis, and bioevaluation of a novel class of (E)-4-oxo-crotonamide derivatives as potent antituberculosis agents
Ren, Jinfeng,Xu, Jian,Zhang, Guoning,Xu, Changliang,Zhao, LiLi,You, XueFu,Wang, Yucheng,Lu, Yu,Yu, Liyan,Wang, Juxian
, p. 539 - 543 (2019/01/09)
A series of novel (E)-4-oxo-2-crotonamide derivatives were designed and synthesized to find potent antituberculosis agents. All the target compounds were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv(MTB). Results reveal that 4-phenyl moiety at part A and short methyl group at part C were found to be favorable. Most of the derivatives displayed promising activity against MTB with MIC ranging from 0.125 to 4 μg/mL. Especially, compound IIIa16 was found to have the best activity with MIC of 0.125 μg/mL against MTB and with MIC in the range of 0.05–0.48 μg/mL against drug-resistant clinical MTB isolates.
Kr?hnke pyridines: Rapid and facile access to Mcl-1 inhibitors
Conlon, Ivie L.,Van Eker, Daniel,Abdelmalak, Sameh,Murphy, William A.,Bashir, Hassan,Sun, Michael,Chauhan, Jay,Varney, Kristen M.,Godoy-Ruiz, Raquel,Wilder, Paul T.,Fletcher, Steven
supporting information, p. 1949 - 1953 (2018/05/04)
The tumorigenic activity of upregulated Mcl-1 is manifested by binding the BH3 α-helical death domains of opposing Bcl-2 family members, neutralizing them and preventing apoptosis. Accordingly, the development of Mcl-1 inhibitors largely focuses on synthe
Substituted 4-oxo-crotonic acid derivatives as a new class of protein kinase B (PknB) inhibitors: synthesis and SAR study
Xu, Changliang,Bai, Xiaoguang,Xu, Jian,Ren, Jinfeng,Xing, Yun,Li, Ziqiang,Wang, Juxian,Shi, Jingjing,Yu, Liyan,Wang, Yucheng
, p. 4763 - 4775 (2017/02/05)
Protein kinase B (PknB) is an essential serine/threonine protein kinase required for Mycobacterium tuberculosis (M. tb) cell division and cell-wall biosynthesis. A high throughput screen using PknB identified a (E)-4-oxo-crotonic acid inhibitor, named YH-8, which was used as a scaffold for SAR investigations. A significant improvement in enzyme affinity was achieved. The results indicated that the α,β-unsaturated ketone scaffold and “trans-” configuration are essential for the activity against PknB. And compounds with an aryl group, especially with electron-withdrawing substituents on benzene ring, exhibited four fold potency than that of YH-8.
Catalytic conjugate addition of indoles to 4-aryl-4-oxobut-2-enoates by FeCl3
Wang, Xiaoxia,Zhang, Yaohong,Xiao, Xiaohui,Li, Xinsheng
supporting information; experimental part, p. 1284 - 1285 (2009/12/03)
The conjugate addition of indoles to 4-aryl-4-oxobut-2-enoates was achieved with FeCl3 as a catalyst under mild conditions. The reaction was highly regioselective and afforded a variety of new 3-substituted indoles in good to excellent yields. Copyright
