Arylcyclopropanecarboxyl Guanidines as Novel, Potent, and Selective Inhibitors of the Sodium Hydrogen Exchanger Isoform-1 was written by Ahmad, Saleem;Doweyko, Lidia M.;Dugar, Sundeep;Grazier, Nyeemah;Ngu, Khehyong;Wu, Shung C.;Yost, Kenneth J.;Chen, Bang-Chi;Gougoutas, Jack Z.;DiMarco, John D.;Lan, Shih-Jung;Gavin, Brian J.;Chen, Alice Y.;Dorso, Charles R.;Serafino, Randy;Kirby, Mark;Atwal, Karnail S.. And the article was included in Journal of Medicinal Chemistry in 2001.Recommanded Product: Methyl 3-bromo-4-fluorobenzoate This article mentions the following:
A novel series of arylcyclopropanecarboxyl guanidines was synthesized and evaluated for activity against the sodium hydrogen exchanger isoform-1 (NHE-1). In biol. assays conducted in an AP1 cell line expressing the human NHE-1 isoform, the starting cyclopropane (IC50 = 3.5 娓璏) shows inhibitory activity comparable to cariporide (IC50 = 3.4 娓璏). Structure-activity relationships are used to optimize the affinity of various acyl guanidines for NHE-1 by screening the effect of substituents at both aryl and cyclopropyl rings. It is demonstrated that introduction of appropriate hydrophobic groups at the Ph ring and a gem-di-Me group at the cyclopropane ring enhances the NHE-1 inhibitory activity by up to 3 orders of magnitude (IC50 = 0.003 娓璏). In addition, the gem-di-Me series of analogs seem to display improved oral bioavailability and longer plasma half-life in rats. Furthermore, the lead benzodihydrofuranyl analog (BMS-284640) shows over 380-fold increased NHE-1 inhibitory activity as well as improved selectivity for NHE-1 over NHE-2 compared to cariporide. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6Recommanded Product: Methyl 3-bromo-4-fluorobenzoate).
Methyl 3-bromo-4-fluorobenzoate (cas: 82702-31-6) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. 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-4-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary