In 2022,Bae, Jinsu; Kim, Yeo-Ok; Han, Xuehao; Yoon, Myung-Ha; Kim, Woong-Mo; Kim, Yong-Chul published an article in Molecules. The title of the article was 《Synthesis and Structure-Activity Relationship Studies of Benzimidazole-4,7-dione-Based P2X3 Receptor Antagonists as Novel Anti-Nociceptive Agents》.Application In Synthesis of 4-Chloro-2-iodoaniline The author mentioned the following in the article:
P2X3 receptors (P2X3R) are ATP-gated ion channels predominantly expressed in C- and Aδ-fiber primary afferent neurons and have been introduced as a novel therapeutic target for neurol. disorders, including neuropathic pain and chronic cough. Because of its localized distribution, antagonism of P2X3R has been thoroughly considered, and the avoidance of issues related to CNS side effects has been proven in clin. trials. In this article, benzimidazole-4,7-dione-based derivatives were introduced as a new chem. entity for the development of P2X3R antagonists. Starting from the discovery of a hit compound from the screening of 8364 random library compounds in the Korea Chem. Bank, which had an IC50 value of 1030 nM, studies of structure-activity and structure-property relationships enabled further optimization toward improving the antagonistic activities as well as the drug′s physicochem. properties, including metabolic stability. As for the results, the final optimized compound 14h was developed with an IC50 value of 375 nM at P2X3R with more than 23-fold selectivity vs. P2X2/3R, along with properties of metabolic stability and improved solubility In neuropathic pain animal models evoked by either nerve ligation or chemotherapeutics in male Sprague-Dawley rats, compound 14h showed anti-nociceptive effects through an increase in the mech. withdrawal threshold as measured by von Frey filament following i.v. administration. After reading the article, we found that the author used 4-Chloro-2-iodoaniline(cas: 63069-48-7Application In Synthesis of 4-Chloro-2-iodoaniline)
4-Chloro-2-iodoaniline(cas: 63069-48-7) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Application In Synthesis of 4-Chloro-2-iodoaniline
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com