Synthesis and Biological Evaluation of New 1,2-Dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for Treatment of Autoimmune Disorders: Structure−Activity Relationship
摘要:
Roquinimex-related 3-quinolinecarboxamide derivatives were prepared and evaluated for treatment of autoimmune disorders. The compounds were tested in mice for their inhibitory effects on disease development in the acute experimental autoimmune encephalomyelitis model and selected compounds in the beagle dog for induction of proinflammatory reaction. Structure-activity relationships are discussed. Compound 8c, laquinimod, showed improved potency and superior toxicological profile compared to the lead compound roquinimex (1b, Linomide) and was selected for clinical studies (currently in phase II).
A method of treating warm-blooded animals suffering from diarrhea, which method comprises the administration of particular 4-(aroylamino)piperidinebutanamide derivatives and compositions containing the same. Novel 4-(aroylamino)piperidinebutanamide derivatives.
Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket
作者:Tianhua Zhang、Zengwei Lai、Suying Yuan、Yi-You Huang、Guoqiang Dong、Chunquan Sheng、Hengming Ke、Hai-Bin Luo
DOI:10.1021/acs.jmedchem.0c00983
日期:2020.9.10
Clinical use of phosphodiesterase-5 (PDE5) inhibitors is limited by several side effects due to weak isoformselectivity. Herein, a unique allosteric pocket of PDE5 is identified by molecular modeling and structural biology, which enables the discovery of highly selective PDE5 inhibitors from natural product evodiamine (EVO). The crystal structure of PDE5 with bound EVO derivative (S)-7e revealed that
Discovery of evodiamine derivatives as potent insecticide candidates
作者:Jingbo Liu、Yabing Shi、Shuting Chen、Fengyun Li、Wen Wen、Yuanhong Wang
DOI:10.1016/j.bmc.2022.116727
日期:2022.5
search for novel more effective insecticides, natural products could be used as ideal template compounds due to their good environmental compatibility, various bioactivities, unique scaffolds and mode of action. We have found that natural product evodiamine, the main active component from the fruits of Evodia rutaecarpa (Juss.) Benth, displayed obvious insecticidal activities against lepidoptera pests
Palladium-catalysed cyclisation of vinylethylene carbonates and anhydrides: a new approach to diverse medium-sized bislactones
作者:Qing-Song Dai、Ying-Mao Tao、Xiang Zhang、Hai-Jun Leng、Hua Huang、Peng Xiang、Qing-Zhu Li、Qi-Wei Wang、Jun-Long Li
DOI:10.1039/d0cc05341d
日期:——
An unprecedented palladium-catalysed regioselective [5 + n] cyclisation (n = 5, 6, and 7) of vinylethylene carbonates and various anhydrides was presented. This protocol could offer a broad spectrum of medium-sized bislactones with skeletal diversity.