21987-27-9Relevant academic research and scientific papers
METHODS AND MATERIALS FOR INCREASING OR MAINTAINING NICOTINAMIDE MONONUCLEOTIDE ADENYLYL TRANSFERASE-2 (NMNAT2) POLYPEPTIDE LEVELS
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, (2020/09/08)
This document provides methods and materials for increasing or maintaining NMNAT2 polypeptide levels within cells. For example, compounds (e.g., organic compounds) having the ability to increase or maintain NMNAT2 polypeptide levels within cells, formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for making formulations containing compounds having the ability to increase or maintain NMNAT2 polypeptide levels within cells, methods for increasing or maintain NMNAT2 polypeptide levels within cells, and methods for treating mammals (e.g., humans) having a condition responsive to an increase in NMNAT2 polypeptide levels are provided (or for preventing said condition).
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
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, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Discovery of carbazole carboxamides as novel RORγt inverse agonists
Huang, Yafei,Yu, Mingcheng,Sun, Nannan,Tang, Ting,Yu, Fazhi,Song, Xiaoxia,Xie, Qiong,Fu, Wei,Shao, Liming,Wang, Yonghui
, p. 465 - 476 (2018/02/28)
A novel series of carbazole carboxamides was discovered as potent RORγt inverse agonists using a scaffold hybridization strategy. Structure-activity relationship exploration on the amide linker, carbazole ring and arylsulfone moiety of the hybrid amide 3a led to identification of potent RORγt inverse agonists. Compound 6c was found to have a good RORγt activity with an IC50 of 58.5 nM in FRET assay, and reasonable inhibitory activity in mouse Th17 cell differentiation assay (58.8% inhibition at 0.3 μM). The binding mode of carbazole carboxamides in RORγt ligand binding domain was discussed.
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists
Page, Daniel,Yang, Hua,Brown, William,Walpole, Christopher,Fleurent, Manon,Fyfe, Meredith,Gaudreault, Francois,St-Onge, Stephane
, p. 6183 - 6187 (2008/04/07)
The preparation and evaluation of a novel class of CB2 agonists based on a 1,2,3,4-tetrahydropyrrolo[3,4-b]indole moiety are reported. They showed binding affinities up to 4.2 nM toward CB2 with sub-nanomolar EC50 values. They also showed moderate to good (>350-fold) selectivity over the CB1 receptor.
Bartoli indole synthesis on solid supports
Knepper, Kerstin,Braese, Stefan
, p. 2829 - 2832 (2007/10/03)
(Matrix presented) Bartoli indole synthesis has been performed for the first time on solid supports. Starting from Merrifield resin, immobilization of five nitro benzoic acids was performed. Addition of four different alkenyl Grignard reagents and basic c
Intramolecular cyclization reactions of unsaturated amino Fischer chromium carbenes forming indoles and quinolines
S?derberg, Bj?rn C. G.,Shriver, James A.,Cooper, Seth H.,Shrout, Timothy L.,Helton, E. Scott,Austin, Lucinda R.,Odens, Herman H.,Hearn, Brian R.,Jones, Paula C.,Kouadio, Tiara N.,Ngi, Tan H.,Baswell, Rachel,Caprara, H. John,Meritt, Mark D.,Mai, Than T.
, p. 8775 - 8791 (2007/10/03)
A thermally induced intramolecular annulation reaction of N-(2-alkenylphenyl)amino substituted Fischer chromium carbenes has been extensively examined. The carbene complexes were prepared in moderate to good yields by reaction of 2-aminostyrenes with intermediately formed acyloxy substituted carbenes. Upon heating, the thermally labile carbenes decomposed producing indoles and quinolines as the major products. The product distribution was found to be highly dependent on the substitution pattern and electronic properties of the starting material, and on the solvent used.
