A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists was written by McKinnell, R. Murray;Armstrong, Scott R.;Beattie, David T.;Choi, Seok-Ki;Fatheree, Paul R.;Gendron, Roland A. L.;Goldblum, Adam;Humphrey, Patrick P.;Long, Daniel D.;Marquess, Daniel G.;Shaw, J. P.;Smith, Jacqueline A. M.;Turner, S. Derek;Vickery, Ross G.. And the article was included in Journal of Medicinal Chemistry in 2009.Product Details of 954-81-4 This article mentions the following:
5-HT4 receptor agonists such as tegaserod have demonstrated efficacy in the treatment of constipation predominant irritable bowel syndrome (IBS-C), a highly prevalent disorder characterized by chronic constipation and impairment of intestinal propulsion, abdominal bloating, and pain. The 5-HT4 receptor binding site can accommodate functionally and sterically diverse groups attached to the amine nitrogen atom of common ligands, occupying what may be termed a “secondary” binding site. Using a multivalent approach to lead discovery, the effects of varying the position and nature of the secondary binding group were investigated as a strategy to achieve the desired 5-HT4 agonist pharmacol. profile. It was shown that the ability of amine-based secondary binding groups to impart exceptional gains in the binding affinity, selectivity, and functional potency of 5-HT4 agonists. Optimization of the leads generated by this approach afforded compound I, a selective, orally efficacious 5-HT4 agonist for the potential treatment of gastrointestinal motility-related disorders. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Product Details of 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon閳ユ彽romine bond is electrophilic, i.e. alkyl bromides are alkylating agents. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Product Details of 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary