Structure and activity relationships of novel uracil derivatives as topical anti-inflammatory agents

Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 – 2014)

“…An issued patent illustrated the representative formula, which is shown as compound (41) ( Table 8); 96 of the example compounds were disclosed to be useful as therapeutic agents for treating various inflammatory diseases that are associated with NE, and their inhibitory IC 50 values were in the nanomolar range (specifically, 3.5 --353.1 nM) [87]. In addition to their utility for the treatment of lung inflammation, topically administered 5-substituted uracil derivatives exerted anti-inflammatory effects on picryl chloride-induced contact hypersensitivity reactions in animals [88] and showed promising results for the treatment of atopic dermatitis and contact dermatitis. In addition, 5-substituted uracil derivatives are suggested as radiation-sensitizing, anticancer and anti-herpes virus agents [89].…”

Synthesis, characterization, fluorescence imaging, and cytotoxicity studies of a uracil‐based azo derivative and its metal complexes

“…The 1 H NMR spectra of the ligand showed a multiplet in the region 7.1-7.97 ppm due to aromatic protons. [24] 13 C NMR spectra of the ligand and the corresponding metal complexes were recorded ( Figure S5 and S6) in DMSO-d 6 . The two nitrogen-hydrogen (NH) groups showed characteristic singlets at δ = 11.7 and 11.8 ppm, which remain unchanged in the complexes.…”

“…The absorption spectra of the ligand show bands at 327 and 487 nm. The spectral bands of Mn(II) are observed at 430 nm and 537 nm, which are assigned to 6 A 1g ! The electronic spectral data of the complexes provide the information regarding the stereochemistry of the metal ion in the complexes.…”

“…These compounds exhibit interesting physical, chemical, photophysical, photochemical, catalytic, and material properties due to their structural behavior, bonding interactions, and metal-binding ability of azo nitrogen. [4] They are also used as antimycobacterial, [5] anti-inflammatory, [6] antibacterial, [7] and antitumor agents. The azo compounds are known for their good thermal stability and excellent optical data storage property.…”

Synthetic applications of benzothiazole containing cyanoacetyl group

“…Acetyl chloride itself is not particularly useful in this respect since it undergoes dimerization [3]. Cyanoacetylation of uracils or their derivatives [4][5][6] and enamines [7] has been reported to be successfully achieved by heating the respective substrate with a mixture of acetic anhydride and cyanoacetic acid as a cyano-acetylating mixture. The structure of the reactive species formed in this case has been assigned as a cyano-ketene.…”