Peiro Cadahia, Jorge published the artcileSynthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis, COA of Formula: C14H21BO3, the publication is Journal of Medicinal Chemistry (2018), 61(8), 3503-3515, database is CAplus and MEDLINE.
A series of novel hydrogen peroxide sensitive prodrugs I (11–13; R = H, Me, F) of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in mice with collagen induced arthritis (CIA) as a model of chronic rheumatoid arthritis (RA). The prodrug strategy selected is based on ROS-labile 4-methylphenylboronic acid promoieties linked to the drugs via a carbamate linkage or a direct C-N bond. Activation under pathophysiol. concentrations of H2O2 proved to be effective, and prodrug candidates were selected in agreement with relevant in vitro physicochem. and pharmacokinetic assays. Selected candidates showed moderate to good solubility, high chem. and enzymic stability, and therapeutic efficacy comparable to the parent drugs in the CIA model. Importantly, the prodrugs displayed the expected safer toxicity profile and increased therapeutic window compared to MTX and AMT while maintaining a comparable therapeutic efficacy, which is highly encouraging for future use in RA patients.
Journal of Medicinal Chemistry published new progress about 1370732-71-0. 1370732-71-0 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester, name is (3-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol, and the molecular formula is C14H21BO3, COA of Formula: C14H21BO3.
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