Microwave Mediated Organic Reaction: A Convenient Approach for Rapid and Efficient Synthesis of Biologically Active Substituted 1,3-Dihydro-2H-indol-2-one Derivatives

Abstract EN

A simple and efficient method has been developed for the synthesis of 1,3-dihydro-2H-indol-2-one derivatives using microwave irradiation technique.

By taking advantage of the efficient source of energy of microwave, compound libraries for lead generation and optimization can be assembled in a fraction of time.

In the present work, first the Schiff’s bases are synthesized by reaction of isatin with substituted anilines in the presence of acetic acid under microwave heating.

Then the condensation of Schiff bases with different secondary amines in the presence of formaldehyde produces Mannich bases.

The newly synthesized Mannich bases were characterized by means of spectral data and then evaluated for anthelmintic activity against Pheretima posthuma (Indian earthworm) and compared with standard albendazole.

The compounds were evaluated at the concentrations of 10, 20, and 50 mg/mL.

The effect of the standard drug albendazole at 10 mg/mL was also evaluated.

The results of the present study indicate that some of the test compounds significantly demonstrated paralysis and also caused death of worms in a dose-dependent manner.