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Human 5-lipoxygenase (5-LOX) is a target for asthma and allergy treatment. Zileuton is the only marketed drug targeting this enzyme (IC50 ∼ 1 μM). The current study identifies a promising lead molecule which could be improved to match the activity of zileuton.

Novel photoactive 4-(4-chlorophenyl)-2-(1H-indol-3-yl)-6-substituted phenyl-2H-thiazolo[3,2-a][1,3,5]triazines were synthesized by the conjugate addition of ammonia to the indole-3-carbaldehyde Schiff bases followed by the condensation with 4-chlorobenzaldehyde. All the synthesized compounds were characterized by FT-IR, NMR, mass spectra and elemental analyses. Their antioxidant property, electrochemical and photophysical properties in different organic solvents were investigated. Comparative discussion on the photophysical properties of indole-3-carbaldehyde Schiff bases and 4-(4-chlorophenyl)-2-(1H-indol-3-yl)-6-substituted phenyl-2H-thiazolo[3,2-a][1,3,5]triazines has been described. The fluorescence quantum yield of Schiff bases (Φf = 0.66-0.70 in DMSO) found to be interestingly higher. High fluorescence quantum yield, large molar extinction coefficient, high stokes shift and smaller optical band gap positioning these new derivatives as an efficient metal free organic fluorescent and semiconductor material. Graphical Abstract ᅟ.

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A novel easy stability indicating high performance liquid chromatography method has been developed for the concurrent assessment of trithioparamethoxy phenylpropene in combination with chlorpheniramine maleate using Luna C8 column with UV detection at 224 nm. The mobile phase comprised of 0.02 N phosphate buffer (pH 5.5) and acetonitrile (55:45 v/v) was delivered with a flow rate of 1.5 mL/min. The method was linear over the concentration range 6.25-18.75 μg/mL (trithioparamethoxy phenylpropene) and 1.5-4.5 μg/mL (chlorpheniramine maleate). The limit of quantification was 1.57 μg/mL (trithioparamethoxy phenylpropene) and 0.969 μg/mL (chlorpheniramine maleate). The calculated recoveries were 100.083-100.287% (trithioparamethoxy phenylpropene) and 99.827-100.277% (chlorpheniramine maleate). Trithioparamethoxy phenylpropene and chlorpheniramine maleate were subjected to forced stress like acid hydrolysis, base hydrolysis, thermal and oxidation degradation. The drugs were found to degrade in the applied conditions. The degraded products were resolved effectively from the trithioparamethoxy phenylpropene and chlorpheniramine maleate. The suggested stability-indicating HPLC method can be used for the quantitative evaluation of trithioparamethoxy phenylpropene and chlorpheniramine maleate in bulk medications and tablet formulations.