27277-67-4

Usage

General Description

1,2,4-Triazine-3,5(2H,4H)-dione, 2-[(3,4-dichlorophenyl)methyl]-, also known as Apremilast, is a medication used for the treatment of inflammatory conditions such as psoriatic arthritis and plaque psoriasis. It works by inhibiting the enzyme phosphodiesterase-4 (PDE4), which plays a role in the inflammation process. By inhibiting this enzyme, the medication helps to reduce the inflammation and associated symptoms. Apremilast is available in tablet form for oral administration and is typically prescribed for long-term use to manage and improve the symptoms of these chronic inflammatory conditions.

Upstream product

• 80305-82-4 C₁₀H₉Cl₂N₃O₃ 
• 102-47-6 3,4-Dichlorophenylmethyl chloride 

Relevant academic research and scientific papers

Anticoccidial derivatives of 6 azauracil. I. Enhancement of activity by benzylation of nitrogen 1. Observations on the design of nucleotide analogues in chemotherapy

Benzylation of 6-azauracil at N-1 (which corresponds to the point of attachment of the ribose phosphate unit in pyrimidine nucleotides) has been found to augment its anticoccidial activity fourfold. The high potency of 1-benzyl-6-azauracil is ascribed to a combination of intrinsic activity, efficient oral absorption, and a moderate rate of excretion. Metabolism experiments using 1-benzyl-6-azauracil labeled with 14C in the heterocycle and (separately) in the side chain showed that, in the drug accounted for, no cleavage had occurred. Additional activity increases were achieved by introducing small, electron-withdrawing substituents in the meta and/or para position(s) of the benzyl group. One of the most active derivatives, 1-(3-cyanobenzyl)-6-azauracil, is about 16 times as potent as 6-azauracil.