4600-04-8Relevant articles and documents
Design, Synthesis, and in Vitro and in Vivo Biological Evaluation of Limonin Derivatives for Anti-Inflammation Therapy
Bian, Ming,Gong, Guohua,Lei, Pang,Du, Huanhuan,Bai, Chunmei,Wei, Chengxi,Quan, Zheshan,Ma, Qianqian
, p. 13487 - 13499 (2021/11/17)
In this study, limonin derivatives were used to design new anti-inflammatory compounds with high pharmacological activity and low toxicity. A total of 23 new limonin derivatives were discovered, synthesized, and screened for their anti-inflammatory activity against lipopolysaccharide (LPS)-treated RAW 264.7 cells. Of them, compound f4 was found to be the most active, with a higher efficiency compared with limonin and celecoxib. Subsequently, we studied the mechanism underlying the activity of f4 and found that it inhibited proinflammatory cytokines by blocking the NF-κB/MAPK signaling pathway in LPS-treated RAW 264.7 cells as well as mice. In conclusion, f4 may be a promising anti-inflammatory lead compound.
Design, synthesis and in-vitro evaluation of fluorinated triazoles as multi-target directed ligands for Alzheimer disease
Dalvi, Tanay,Dewangan, Bhaskar,Agarwal, Gopal,Shinde Suchita, Dattatray,Jain, Alok,Srivastava, Akshay,Sahu, Bichismita
, (2021/04/27)
Alzheimer disease is multi-factorial and inflammation plays a major role in the disease progression and severity. Metals and reactive oxygen species (ROS) are the key mediators for inflammatory conditions associated with Alzheimer's. Along multi-factorial nature, major challenge for developing new drug is the ability of the molecule to cross blood brain barrier (BBB). We have designed and synthesized multi-target directed hexafluorocarbinol containing triazoles to inhibit Amyloid β aggregation and simultaneously chelate the excess metals present in the extracellular space and scavenge the ROS thus reduce the inflammatory condition. From the screened compound library, compound 1c found to be potent and safe. It has demonstrated inhibition of Amyloid β aggregation (IC50 of 4.6 μM) through selective binding with Amyloid β at the nucleation site (evidenced from the molecular docking). It also chelate metals (Cu+2, Zn+2 and Fe+3) and scavenges ROS significantly. Due to the presence of hexafluorocarbinol moiety in the molecule it may assist to permeate BBB and improve the pharmacokinetic properties. The in-vitro results of compound 1c indicate the promiscuity for the development of hexafluorocarbinol containing triazoles amide scaffold as multi-target directed therapy against Alzheimer disease.
Co-catalyst and solvent free nitrogen rich triazole based organocatalysts for cycloaddition of CO2 into epoxide
Elkadi, Mirella,Khattak, Zafar A. K.,Suleman, Suleman,Ullah, Habib,Verpoort, Francis,Younus, Hussein A.
, (2020/07/21)
A general synthesis of triazole-based catalysts remains a significant challenge. Consequently, triazole-based catalysts are rarely studied. Herein, the first report is presented for the construction of cyclic carbonates using triazole-based organocatalyst
