Son, Jung-Ho; Phuan, Puay-Wah; Zhu, Jie S.; Lipman, Elena; Cheung, Amy; Tsui, Ka Yi; Tantillo, Dean J.; Verkman, Alan S.; Haggie, Peter M.; Kurth, Mark J. published an article in European Journal of Medicinal Chemistry. The title of the article was 《1-Benzylspiro[piperidine-4,1′-pyrido[3,4-b]indole] ‘co-potentiators’ for minimal function CFTR mutants》.Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene The author mentioned the following in the article:
A spiro [piperidine-4,1-pyrido [3,4-b]indoles] I (R1 = 6-OMe, 6-Br, 6-Cl, 7-OMe; R2 = benzyl, furan-2-ylmethyl, pyridin-2-ylmethyl, etc.) class of co-potentiators that function in synergy with existing CFTR potentiators such as VX-770 or GLGP1837 to restore channel activity of a defined subset of minimal function cystic fibrosis transmembrane conductance regulator (CFTR) mutants has been described. Here, structure-activity studies were conducted to improve their potency over the previously identified compound, I (R1 = 6-OMe; R2 = benzyl) 20 (originally termed CP-A01). Targeted synthesis of 37 spiro [piperidine-4,1-pyrido [3,4-b]indoles] I was generally accomplished using versatile two or three step reaction protocols with each step having high efficiency. Structure-activity relationship studies established that analog I [R1 = 6-OMe; R2 = (2,4,5-trifluorophenyl)methyl], with 6′-methoxyindole and 2,4,5-trifluorobenzyl substituents, had the greatest potency for activation of N1303K-CFTR, with EC50 ∼600 nM representing an ∼17-fold improvement over the original compound identified in a small mol. screen.4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene) was used in this study.
4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Recommanded Product: 4-Bromo-1-(bromomethyl)-2-fluorobenzene In contrast, terrestrial plants account only for a few bromine-containing compounds.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary