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Synthesis and antimicrobial evaluation of purine substituted N-acyl-α-carboxamides via the Ugi four-component reaction

Abstract A series of novel purine based N-acyl-α-carboxamides were prepared via the Ugi four-component reaction approach using the pharmacophoric 2-amino-6-chloropurine moiety as the amine component coupled with various aldehydes, carboxylic acids and isocyanides affording a library of multisubstituted compounds 2a–x. These compounds were screened for their antimicrobial activity against Gram negative strains Escherichia coli, Pseudomonas aeruginosa and Gram positive strains Staphylococcus aureus, Staphylococcus epidermidis demonstrating significant biological potency. The best potency for all the strains was found for compound 2x, which is comparable with ampicillin trihydrate as the standard drug.