Pharmacological Assessment of Ugi Multicomponent Reaction: Rapid and Green Synthesis of Novel Biological Agents

Abstract

In this article, we report a novel, rapid and facile synthesis of a series of azo coupled Ugi four-component reaction derivatives and its evaluation for biological activity. A general and straightforward approach towards the microwaveassisted synthesis was initiated by the condensation reaction to obtain compounds 5 (a-h) achieving 80-92% yields. The reactions were irradiated for 5-10 min in presence of fluorite catalyst. The resulting compounds were diazotized followed by coupling reaction to attain compounds 7 (a-h) with 65-74% yields. The synthesized compounds were characterized on the basis of 1H and 13C NMR, I.R, elemental analysis, and mass spectral data. All the synthesized derivatives 7 (a-h) were screened for their potential in vivo anti-inflammatory action against a reference drug, Diclofenac. These compounds were also screened for in vitro antimicrobial activity against a few Gram- positive and Gram-negative bacteria using reference antibiotics, Ampicillin and Streptomycin. The screening data revealed that compounds 7g and 7h possess potential antiinflammatory activity while compounds 7a, 7b, 7g and 7h show potent antimicrobial activity. Structural variations bring about new physical and biological properties. As a result, azo coupled Ugi-4CR derivatives in near future can be used as potent drugs for inflammation and bacterial infections.