Oxindole

Oxindole is an aromatic heterocyclic building block. 2-indolinone derivatives have become lead compounds in the research of kinase inhibitors.Oxindole structure has been used in receptor tyrosine kinases (RTKs) inhibitors such as SU4984 and intedanib, the RTK family represents an important therapeutic target for anti-cancer drug development.We synthesized a series of novel 5-24 derivatives of Oxindole. METHODS AND RESULTS: The synthesis started from 5-chloroOxindole, which was condensed with methyl 4-carboxybezoate and result in the formation of benzolyester derivatives of Oxindole which was then treated with hydrazine hydrate. The Oxindole benzoylhydrazide was treated with aryl acetophenones and aldehydes to get target compounds 5-24. The synthesized compounds were evaluated for urease inhibition; the compound 5 (IC50 = 13.00 ± 0.35 μM) and 11 (IC50 = 19.20 ± 0.50 μM) showed potent activity as compared to the standard drug thiourea (IC50 = 21.00 ± 0.01 μM) . Other compounds showed moderate to weak activity.