3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17 was written by Baqi, Younis;Pillaiyar, Thanigaimalai;Abdelrahman, Aliaa;Kaufmann, Olesja;Alshaibani, Samer;Rafehi, Muhammad;Ghasimi, Saman;Akkari, Rhalid;Ritter, Kirsten;Simon, Katharina;Spinrath, Andreas;Kostenis, Evi;Zhao, Qiang;Kose, Meryem;Namasivayam, Vigneshwaran;Muller, Christa E.. And the article was included in Journal of Medicinal Chemistry in 2018.Application of 660-49-1 This article mentions the following:
The orphan receptor GPR17 may be a novel drug target for inflammatory diseases. 3-(2-Carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid (MDL29,951, 1) was previously identified as a moderately potent GPR17 agonist. In the present study, we investigated the structure-activity relationships (SARs) of 1. Substitution of the indole 1-, 5-, or 7-position was detrimental. Only small substituents were tolerated in the 4-position while the 6-position accommodated large lipophilic residues. Among the most potent compounds were 3-(2-carboxyethyl)-1H-indole-2-carboxylic acid derivatives containing the following substituents: 6-phenoxy (26, PSB-1737, EC50 270 nM), 4-fluoro-6-bromo (33, PSB-18422, EC50 27.9 nM), 4-fluoro-6-iodo (35, PSB-18484, EC50 32.1 nM), and 4-chloro-6-hexyloxy (43, PSB-1767, EC50 67.0 nM). (3-(2-Carboxyethyl)-6-hexyloxy-1H-indole-2-carboxylic acid (39, PSB-17183, EC50 115 nM) behaved as a partial agonist. Selected potent compounds tested at human P2Y receptor subtypes showed high selectivity for GPR17. Docking into a homol. model of the human GPR17 and mol. dynamic simulation studies rationalized the observed SARs. In the experiment, the researchers used many compounds, for example, 3-Fluoro-5-iodoaniline (cas: 660-49-1Application of 660-49-1).
3-Fluoro-5-iodoaniline (cas: 660-49-1) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. Organoiodine lubricants can be used with titanium, stainless steels, and other metals which tend to seize up with conventional lubricants: organoiodine lubricants can be used in turbines and spacecraft, and as a cutting oil in machining.Application of 660-49-1
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com