Discovery of Novel 5-(Piperazine-1-carbonyl)pyridin-2(1H)-one Derivatives as Orally eIF4A3-Selective Inhibitors was written by Mizojiri, Ryo;Nakata, Daisuke;Satoh, Yoshihiko;Morishita, Daisuke;Shibata, Sachio;Iwatani-Yoshihara, Misa;Kosugi, Yohei;Kosaka, Mai;Takeda, Junpei;Sasaki, Shigekazu;Takami, Kazuaki;Fukuda, Koichiro;Kamaura, Masahiro;Sasaki, Shinobu;Arai, Ryosuke;Cary, Douglas R.;Imaeda, Yasuhiro. And the article was included in ACS Medicinal Chemistry Letters in 2017.Application In Synthesis of 5-Bromo-6-methoxynicotinic acid This article mentions the following:
Starting from our previous eIF4A3-selective inhibitor I, a novel series of (piperazine-1-carbonyl)pyridin-2(1H)-one derivatives was designed, synthesized, and evaluated for identification of orally bioavailable probe mols. Compounds II and III showed improved physicochem. and ADMET profiles, while maintaining potent and subtype-selective eIF4A3 inhibitory potency. In accord with their promising PK profiles and results from initial in vivo PD studies, compounds II and III showed antitumor efficacy with T/C values of 54% and 29%, resp., without severe body weight loss. Thus, our novel series of compounds represents promising probe mols. for the in vivo pharmacol. study of selective eIF4A3 inhibition. In the experiment, the researchers used many compounds, for example, 5-Bromo-6-methoxynicotinic acid (cas: 1186194-46-6Application In Synthesis of 5-Bromo-6-methoxynicotinic acid).
5-Bromo-6-methoxynicotinic acid (cas: 1186194-46-6) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.Application In Synthesis of 5-Bromo-6-methoxynicotinic acid
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary