Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model was written by Liang, Jun;Van Abbema, Anne;Balazs, Mercedesz;Barrett, Kathy;Berezhkovsky, Leo;Blair, Wade S.;Chang, Christine;Delarosa, Donnie;De Voss, Jason;Driscoll, Jim;Eigenbrot, Charles;Goodacre, Simon;Ghilardi, Nico;MacLeod, Calum;Johnson, Adam;Bir Kohli, Pawan;Lai, Yingjie;Lin, Zhonghua;Mantik, Priscilla;Menghrajani, Kapil;Nguyen, Hieu;Peng, Ivan;Sambrone, Amy;Shia, Steven;Smith, Jan;Sohn, Sue;Tsui, Vickie;Ultsch, Mark;Williams, Karen;Wu, Lawren C.;Yang, Wenqian;Zhang, Birong;Magnuson, Steven. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.HPLC of Formula: 1334411-79-8 The following contents are mentioned in the article:
Herein we report identification of an imidazopyridine class of potent and selective TYK2 inhibitors, exemplified by prototype 6, through constraint of the rotatable amide bond connecting the pyridine and aryl rings of compound 1. Further optimization led to generation of compound 30 that potently inhibits the TYK2 enzyme and the IL-23 pathway in cells, exhibits selectivity against cellular JAK2 activity, and has good pharmacokinetic properties. In mice, compound 30 demonstrated dose-dependent reduction of IL-17 production in a PK/PD model as well as in an imiquimod-induced psoriasis model. In this efficacy model, the IL-17 decrease was accompanied by a reduction of ear thickness indicating the potential of TYK2 inhibition as a therapeutic approach for psoriasis patients. This study involved multiple reactions and reactants, such as 4-Bromo-2-(2,6-dichlorophenyl)-1H-imidazo[4,5-c]pyridine (cas: 1334411-79-8HPLC of Formula: 1334411-79-8).
4-Bromo-2-(2,6-dichlorophenyl)-1H-imidazo[4,5-c]pyridine (cas: 1334411-79-8) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.HPLC of Formula: 1334411-79-8
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem