New saccharin derivatives as tyrosinase inhibitors

In vitroinhibition effect and structure–activity relationships of some saccharin derivatives on erythrocyte carbonic anhydrase I and II

“…6-(Phenylurenyl/thiourenyl) saccharin compounds (6a-v) were synthesized from 4-nitrotoluene (1) in five steps by known procedures 12 .…”

“…It has been observed that their potency varied between 3.3 and 226 nM, and by means of X-ray crystallography a highly variable orientation of the R-ureido moieties was evidenced when the inhibitor was bound within the enzyme active site 11 . In this study, we evaluated 6-(phenylurenyl/thiourenyl) saccharin derivatives (6a-v), synthesized in the previous work 12 , effects on hCA I and hCA II purified from human erythrocytes. Additionally, we presented SAR analyses.…”

Synthesis, antioxidant and anticholinesterase activities of novel coumarylthiazole derivatives

“…These studies have reported that a hydrogen bond has been formed between amid moieties of the inhibitors and anionic sites of the enzyme [25,26]. The urea group was chosen on the basis of its potency of H-bonding, probability of complexation and wide biological activity [27][28][29][30]. We report here a new hybrid molecule (1) based on frameworks of the coumarin modified by the addition of thiazole ring (Fig.…”

Synthesis, Biological Activity and Structure‐Activity Relationship of Novel Diphenylurea Derivatives Containing Tetrahydroquinoline as Carbonic Anhydrase I and II Inhibitors

“…As seen in this, the target compounds (7 a-t) were synthesized by four steps including modified condensation, addition and ring closing reactions. [50][51][52] All synthesized compounds were characterized by Nuclear Magnetic Resonance Spectroscopy ( 1 H-NMR, 13 C-NMR) and Fourier Transform Infrared Spectroscopy (FTIR). Then structures of 6 a-t and 7 a-t were also confirmed by High Pressure Liquid Chromatography -Time of Flight / Mass Spectroscopy (HPLC-ToF/MS).…”