887982-16-3Relevant academic research and scientific papers
Picolinamide compound and preparation method and application thereof
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Paragraph 0073; 0075; 0096-0100; 0165; 0167; 0172-0175, (2020/08/02)
The invention discloses a picolinamide compound. The structural general formulas of the picolinamide compound are shown as formulas (I) and (II). The invention also discloses a preparation method of the picolinamide compound and application of the picolinamide compound in preparation of anti-tumor drugs. The picolinamide compound can effectively inhibit a variety of tumor cells, including human breast cancer cells, human lung cancer cells, human liver cancer cells and the like, has good anti-tumor active substances and can be used for preparing the anti-tumor drugs.
Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives
Kort, Michael E.,Atkinson, Robert N.,Thomas, James B.,Drizin, Irene,Johnson, Matthew S.,Secrest, Matthew A.,Gregg, Robert J.,Scanio, Marc J.C.,Shi, Lei,Hakeem, Ahmed H.,Matulenko, Mark A.,Chapman, Mark L.,Krambis, Michael J.,Liu, Dong,Shieh, Char-Chang,Zhang, Xufeng,Simler, Gricelda,Mikusa, Joseph P.,Zhong, Chengmin,Joshi, Shailen,Honore, Prisca,Roeloffs, Rosemarie,Werness, Stephen,Antonio, Brett,Marsh, Kennan C.,Faltynek, Connie R.,Krafte, Douglas S.,Jarvis, Michael F.,Marron, Brian E.
scheme or table, p. 6812 - 6815 (2011/01/04)
A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Nav1.8 sodium channel is reported. Replacement of the furan nucleus and homologation of the anilide linker in subtype-selective blocker A-803467 (1) provided potent, selective derivatives with improved aqueous solubility and oral bioavailability. Representative compounds from this series displayed efficacy in rat models of inflammatory and neuropathic pain.
