Synthesis of eosinophil infiltration inhibitors with antihistaminic activity was written by Gyoten, Michiyo;Nagaya, Hideaki;Fukuda, Shigeru;Ashida, Yasuko;Kawano, Yasuhiko. And the article was included in Chemical & Pharmaceutical Bulletin in 2003.Computed Properties of C4H8ClI This article mentions the following:
A series of [1,2,4]triazolo[1,5-b]pyridazines and imidazo[1,2-b]pyridazines having cyclic amines was synthesized and evaluated for antihistaminic activity and inhibitory effect on eosinophil infiltration. When a piperidine or a piperazine containing a benzhydryl group and a suitable spacer was incorporated at the 6-position, the fused pyridazines were found to exhibit both antihistaminic activity and an inhibitory effect on eosinophil chemotaxis. Above all, one product showed potent antihistaminic activity, but little blockade of central H1 receptors in contrast with its complete blockade of peripheral H1 receptors as determined by an ex vivo binding assay. Furthermore, the same product inhibited eosinophil infiltration of the skin caused by a topical antigen challenge in sensitized guinea pigs, while an antihistamine terfenadine was not effective. After the pharmacokinetic study, this product was found to be rapidly hydrolyzed to 2-[6-[[3-[4-(diphenylmethoxy)-piperidino]propyl]amino]imidazo [1,2-b]pyridazin-2-yl]-2-methylpropionic acid dihydrate (TAK-427), which was also orally active. The later product having both antihistaminic and antiinflammatory activity, is currently undergoing clin. trials as a therapeutic agent for atopic dermatitis and allergic rhinitis. In the experiment, the researchers used many compounds, for example, 1-Chloro-4-iodobutane (cas: 10297-05-9Computed Properties of C4H8ClI).
1-Chloro-4-iodobutane (cas: 10297-05-9) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Polyiodoorganic compounds are sometimes employed as X-ray contrast agents, in fluoroscopy, a type of medical imaging. This application exploits the X-ray absorbing ability of the heavy iodine nucleus.Computed Properties of C4H8ClI
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com