Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers.
Hogendorf AS, Hogendorf A, Popiołek-Barczyk K, Ciechanowska A, Mika J, Satała G, Walczak M, Latacz G, Handzlik J, Kieć-Kononowicz K, Ponimaskin E, Schade S, Zeug A, Bijata M, Kubicki M, Kurczab R, Lenda T, Staroń J, Bugno R, Duszyńska B, Pilarski B, Bojarski AJ.
Hogendorf AS, et al.
Eur J Med Chem. 2019 May 15;170:261-275. doi: 10.1016/j.ejmech.2019.03.017. Epub 2019 Mar 11.
Eur J Med Chem. 2019.
PMID: 30904783
A potent and drug-like agonist, 3-(1-ethyl-1H-imidazol-5-yl)-5-iodo-4-fluoro-1H-indole (AGH-192, 35, K(i 5-HT7)(R) = 4 nM), was identified by optimizing the halogen bond formation with Ser5.42 as the supposed partner. ...
A potent and drug-like agonist, 3-(1-ethyl-1H-imidazol-5-yl)-5-iodo-4-fluoro-1H-indole (AGH-192, 35, K(i 5-HT7)(R) = 4 nM), was ident …