Akiu, Mayuko; Tsuji, Takashi; Sogawa, Yoshitaka; Terayama, Koji; Yokoyama, Mika; Tanaka, Jun; Asano, Daigo; Sakurai, Ken; Sergienko, Eduard; Sessions, E. Hampton; Gardell, Stephen J.; Pinkerton, Anthony B.; Nakamura, Tsuyoshi published an article in 2021. The article was titled 《Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.HPLC of Formula: 847818-74-0 The information in the text is summarized as follows:
Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step of the NAD+ salvage pathway. Since NAD+ plays a pivotal role in many biol. processes including metabolism and aging, activation of NAMPT is an attractive therapeutic target for treatment of diverse array of diseases. Herein, we report the continued optimization of novel urea-containing derivatives which were identified as potent NAMPT activators. Early optimization of HTS hits afforded compound 12 (I) , with a triazolopyridine core, as a lead compound CYP direct inhibition (DI) was identified as an issue of concern, and was resolved through modulation of lipophilicity to culminate in 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea (21, II), which showed potent NAMPT activity accompanied with attenuated CYP DI towards multiple CYP isoforms. The results came from multiple reactions, including the reaction of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0HPLC of Formula: 847818-74-0)
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. HPLC of Formula: 847818-74-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics