Oxazolones: New tyrosinase inhibitors; synthesis and their structure–activity relationships

The tyrosinase inhibitory potential of seventeen synthesized oxazolone derivatives has been evaluated and their structure–activity relationships developed in the present work

Khalid Mohammed Khan

2006

Scholarcy highlights

  • The tyrosinase inhibitory potential of seventeen synthesized oxazolone derivatives has been evaluated and their structure–activity relationships developed in the present work
  • Compounds 3, 9–11, 13, 14, 16, 17, and 19 were found to be better than kojic acid but not l-mimosine.-3-phenyl-2-propenyliden]-1,3-oxazol-5(4H)-one bearing a cinnamyol residue at C-4 of oxazolone moiety and an IC50 = 1.23 ± 0.37 μM was found to be the most active one among all tested compounds. These studies reveal that the substitution of functional group at C-4 and C-2 positions plays a vital role in the activity of this series of compounds
  • It is concluded that compound 7 may act as a potential lead molecule to develop new drugs for the treatment of tyrosinase based disorders

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