Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 1032350-13-2, Name is MK-2206 Dihydrochloride, SMILES is O=C1NN=C2C3=C(N=C(C4=CC=C(C5(N)CCC5)C=C4)C(C6=CC=CC=C6)=C3)C=CN21.[H]Cl.[H]Cl, belongs to indole-building-block compound. In a document, author is Jia, Fang, introduce the new discover, SDS of cas: 1032350-13-2.
Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors
Aiming to develop novel ATX inhibitors, an indole-3-carboxylic acid lead Indole-1 was identified through high-throughput screening (HTS) efforts. The Indole-1 analogs 1-7 was firstly prepared which exerted mild activity comparable to Indole-1 (740 nM) in ATX enzyme assay. Further structural modification to identify type IV ATX inhibitors was proceeded through derivatization of the indole-3-carboxylic acid group. Resultantly, compounds 8-17 containing acyl hydrazone linker displayed poor activity (over 3.49 mu M). Alternatively, replacing the acylhydrazone linker with urea counterpart by the amide bond reversal principle, the acquired compounds 18-22 achieved obvious improvements with submicromolar activities. Furthermore, with the aim to reducing cLogP, the thiazole ring of 18-22 was altered to the benzamide (23-32) with the urea linker unchanged. Remarkably, the benzamide derivative 24 with 4-hydroxy piperidine fragment was identified which exhibited prominent activity with IC50 value of 2.3 nM. Especially, dedicated molecular docking study was throughout the modification process which qualified 24 as optimal entity in accordance with the ATX inhibitory results.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 1032350-13-2 is helpful to your research. SDS of cas: 1032350-13-2.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles