Son, Jung-Ho published the artcile1-Benzylspiro[piperidine-4,1′-pyrido[3,4-b]indole] ‘co-potentiators’ for minimal function CFTR mutants, Application In Synthesis of 76283-09-5, the publication is European Journal of Medicinal Chemistry (2021), 112888, database is CAplus and MEDLINE.
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.
European Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C28H29NO4, Application In Synthesis of 76283-09-5.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary