Design, synthesis, characterization, and antimicrobial activity of biginelli products of indandione

Abstract

A simple and efficient method has been developed for the synthesis of 4-(substituted phenyl)-3,4-dihydro-1H-indeno [1,2-d] pyrimidine-2,5-dione (5) and 4-(substituted phenyl)-2-thioxo-1,2,3,4-tetrahydroindeno [1,2-d] pyrimidine-5-one (6), by a one-pot three component cyclocondensation reaction of 1,3 dicarbonyl compound (Indandione) (1), aromatic aldehyde (2), and urea/thiourea (3/4) using catalytic amount of conc. HCl in refluxing ethanol. Representative samples were screened for their antimicrobial activity against gram-negative bacteria, E coli and Paeruginosa and gram-positive bacteria, S aureus, and C diphtheriae using disc diffusion method. The structures of the products were confirmed by IR, 1H, 13C NMR, and elemental analysis. © 2012 HeteroCorporation.