Synthesis of pyrazolo[4,3-e][1,2,4]triazine sulfonamides, novel Sildenafil analogs with tyrosinase inhibitory activity

Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity

“…Phenolic hydroxyl groups are generally capable to coordinate copper atoms causing inhibition of the enzyme in competition to the catechol substrate. However, our previous study 10 showed that inhibitors with NH group in the sulfonamide part (as piperazinyl, homopiperazinyl) are more active as they reduce the enzyme activity of tyrosinase to 29.5%–33.5%. It was suggested, that NH or free NH 2 group are involved in the inhibition effect of tyrosinase activity.…”

“…They possess various types of pharmacological activities such as antibacterial, high-ceiling diuretic, hypoglycemic, antithyroid, anti-inflammatory and antiglaucoma 1–9 . Moreover, numerous sulfonamides were found to act as tyrosinase and urease inhibitors 10–12 .…”

Development of actinobacterial resources for functional cosmetics

“…The IC 50 values for Distylium racemosum Sieb. et Zucc extracts, triazine sulfonamides, green tea components, and extracted flavonoids from Helichrysum teretifolium were found to be 27.1 μg mL −1 , 0.07‐0.15 μg mL −1 , 17.34 μmol L −1 , and 8.092 μg mL −1 , respectively. IC 50 values for the compounds produced by Streptomyces bikiniensis were greater than 200 μg mL −1 .…”

Relaxant effects of selected sildenafil analogues in the rat aorta

“…Compound (8a) was the most active, with IC 50 values comparable with that one of IBMX. It may be related to its chemical structure and similarity to sildenafil 15 . Other compounds and different sildenafil chemical modifications turned to be less active regarding their vasorelaxant properties.…”