863289-90-1Relevant academic research and scientific papers
Design and synthesis of the first indole-based blockers of Panx-1 channel
Crocetti, Letizia,Guerrini, Gabriella,Puglioli, Sara,Giovannoni, Maria Paola,Di Cesare Mannelli, Lorenzo,Lucarini, Elena,Ghelardini, Carla,Wang, Junjie,Dahl, Gerhard
, (2021/06/28)
Panx-1 is a membrane channel protein involved in some pathologies such as ischemic stroke, cancer and neuropathic pain, thus representing a promising therapeutic target. We present here a study aimed at obtaining the first class of selective Panx-1 blocke
Synthesis and SAR of 2-carboxylic acid indoles as inhibitors of plasminogen activator inhibitor-1
Hu, Baihua,Jetter, James W.,Wrobel, Jay E.,Antrilli, Thomas M.,Bauer, Jean S.,Di, Li,Polakowski, Sergiusz,Jain, Uday,Crandall, David L.
, p. 3514 - 3518 (2007/10/03)
We synthesized and evaluated a novel series of 2-carboxylic acid indole-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). Systematic modification of the N-1 position and the 5-position of the indole scaffold resulted in the identification of several compounds that showed good potency against PAI-1 in the spectrophotometric assay. This potency did not always translate to the antibody assay. Solubility and serum protein binding studies on selected analogs revealed that protein binding might be a factor in the poor correlation between the two assays.
