452349-52-9Relevant academic research and scientific papers
Inhibition of human dhodh by 4-hydroxycoumarins, fenamic acids, and n-(alkylcarbonyl)anthranilic acids identified by structure-guided fragment selection
Fritzson, Ingela,Svensson, Bo,Al-Karadaghi, Salam,Walse, Bjoern,Wellmar, Ulf,Nilsson, Ulf J.,Da Graca Thrige, Dorthe,Joensson, Stig
, p. 608 - 617 (2010)
A strategy that combines virtual screening and structureguided selection of fragments was used to identify three unexplored classes of human DHODH inhibitor compounds: 4-hydroxycoumarins, fenamic acids, and N-(alkylcarbonyl) anthranilic acids. Structure-guided selection of fragments targeting the inner subsite of the DHODH ubiquinone binding site made these findings possible with screening of fewer than 300 fragments in a DHODH assay. Fragments from the three inhibitor classes identified were subsequently chemically expanded to target an additional subsite of hydrophobic character. All three classes were found to exhibit distinct structure-activity relationships upon expansion. The novel N-(alkylcarbonyl)anthranilic acid class shows the most promising potency against human DHODH, with IC50 values in the low nanomolar range. The structure of human DHODH in complex with an inhibitor of this class is presented.
DHODH INHIBITORS AND THEIR USE AS ANTIVIRAL AGENTS
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Page/Page column 58, (2020/11/22)
The present invention relates to a compound, or a dimer or a pharmaceutically acceptable salt or solvate of said compound or dimer, for use in a method for the treatment of a disease, disorder or condition caused by an RNA virus, said compound having the general structure shown in Formula (I).
NEW COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE THEREOF
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Page/Page column 32, (2010/02/13)
Compounds of formula (I), for clinical treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition comprising a compound of formula (I) in an amount giving a daily dosage of from 0.005 mg/kg to 10 mg/kg body weight, in particular from 0.025 mg/kg to 2 mg/kg body weight.
