Bremer, Paul T. published the artcilePicolinic acids as β-exosite inhibitors of botulinum neurotoxin A light chain, Quality Control of 1256358-95-8, the publication is Chemical Communications (Cambridge, United Kingdom) (2016), 52(84), 12521-12524, database is CAplus and MEDLINE.
In developing small-mol. inhibitors of botulinum neurotoxin serotype A light chain (BoNT/A LC), substituted picolinic acids were identified. Extensive investigation into the SAR of the picolinic acid scaffold revealed 5-(1-butyl-4-chloro-1H-indol-2-yl)picolinic acid (I), which possessed low micromolar activity against BoNT/A. Kinetic and docking studies demonstrated binding of I to the β-exosite: a largely unexplored site on the LC that holds therapeutic relevance for botulism treatment.
Chemical Communications (Cambridge, United Kingdom) published new progress about 1256358-95-8. 1256358-95-8 belongs to indole-building-block, auxiliary class Indole,Chloride,Boronic acid and ester,Boronic Acids,Boronate Esters, name is 4-Chloro-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole, and the molecular formula is C14H17BClNO2, Quality Control of 1256358-95-8.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles