53475-34-6Relevant articles and documents
Nitrogen-Centered Concave Molecules with Double Fused Pentagons
Deng, Niping,Zhang, Gang
, p. 5248 - 5251 (2019)
Distinctive concave compounds bearing a nitrogen core and double fused pentagons were synthesized with a palladium-catalyzed intramolecular coupling of 1-chloro-8H-indolo[3,2,1-de]acridine as the key step. Structural analysis confirmed the formation of bo
Catalytic Oxidative Coupling Cyclization for Construction of Benzofuroindolenines under Mild Reaction Conditions
Lin, Yuqi,Ye, Jinxiang,Zhang, Wenting,Gao, Yu,Chen, Haijun
supporting information, p. 432 - 435 (2018/12/13)
We describe iron-catalyzed oxidative coupling cyclization of tetrahydrocarbazoles or THβCs or THγCs to form benzofuroindolenines as fused polycyclic indoles. This mild, efficient and simple approach afforded a library of more than 52 complex compounds across a range of substrate classes with good to excellent yields. (Figure presented.).
Discovery of lead compounds targeting the bacterial sliding clamp using a fragment-based approach
Yin, Zhou,Whittell, Louise R.,Wang, Yao,Jergic, Slobodan,Liu, Michael,Harry, Elizabeth J.,Dixon, Nicholas E.,Beck, Jennifer L.,Kelso, Michael J.,Oakley, Aaron J.
supporting information, p. 2799 - 2806 (2014/04/17)
The bacterial sliding clamp (SC), also known as the DNA polymerase III β subunit, is an emerging antibacterial target that plays a central role in DNA replication, serving as a protein-protein interaction hub with a common binding pocket to recognize linear motifs in the partner proteins. Here, fragment-based screening using X-ray crystallography produced four hits bound in the linear-motif-binding pocket of the Escherichia coli SC. Compounds structurally related to the hits were identified that inhibited the E. coli SC and SC-mediated DNA replication in vitro. A tetrahydrocarbazole derivative emerged as a promising lead whose methyl and ethyl ester prodrug forms showed minimum inhibitory concentrations in the range of 21-43 μg/mL against representative Gram-negative and Gram-positive bacteria species. The work demonstrates the utility of a fragment-based approach for identifying bacterial sliding clamp inhibitors as lead compounds with broad-spectrum antibacterial activity.