Synthesis of novel benzbromarone derivatives designed to avoid metabolic activation.
Basic Information
ID: ALA4325877
Journal: Bioorg Med Chem Lett
Title: Synthesis of novel benzbromarone derivatives designed to avoid metabolic activation.
Authors: Ohe T, Umezawa R, Kitagawara Y, Yasuda D, Takahashi K, Nakamura S, Abe A, Sekine S, Ito K, Okunushi K, Morio H, Furihata T, Anzai N, Mashino T.
Abstract: We synthesized six novel BBR derivatives that were designed to avoid metabolic activation via ipso-substitution and evaluated for their degree of toxicity and hURAT1 inhibition. It was found that all of the derivatives demonstrate lower cytotoxicity in mouse hepatocytes and lower levels of metabolic activation than BBR, while maintaining their inhibitory activity toward the uric acid transporter. We propose that these derivatives could serve as effective uricosuric agents that have much better safety profiles than BBR.
CiteXplore: 30389287
DOI: 10.1016/j.bmcl.2018.10.023
Patent ID: ┄