Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development was written by Raboisson, Patrick;Breitholtz-Emanuelsson, Anna;Dahlloef, Henrik;Edwards, Louise;Heaton, William L.;Isaac, Methvin;Jarvie, Keith;Kers, Annika;Minidis, Alexander B. E.;Nordmark, Anna;Sheehan, Susan M.;Slassi, Abdelmalik;Stroem, Peter;Terelius, Ylva;Wensbo, David;Wilson, Julie M.;Xin, Tao;McLeod, Donald A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Recommanded Product: Methyl 3-bromo-5-fluorobenzoate This article mentions the following:
AZD9272 and AZD6538 are two novel mGluR5 neg. allosteric modulators selected for further clin. development. An initial high-throughput screening revealed leads with promising profiles, which were further optimized by minor, yet indispensable, structural modifications to bring forth these drug candidates. Advantageously, both compounds may be synthesized in as little as one step. Both are highly potent and selective for the human as well as the rat mGluR5 where they interact at the same binding site than MPEP. They are orally available, allow for long interval administration due to a high metabolic stability and long half-lives in rats and permeate the blood brain barrier to a high extent. AZD9272 has progressed into phase I clin. studies. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-5-fluorobenzoate (cas: 334792-52-8Recommanded Product: Methyl 3-bromo-5-fluorobenzoate).
Methyl 3-bromo-5-fluorobenzoate (cas: 334792-52-8) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon鑱砨romine bond is electrophilic in nature. 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.Recommanded Product: Methyl 3-bromo-5-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary