Identification of novel imidazoles as IDO1 inhibitors through microwave-assisted one-pot multicomponent reactions

A series of imidazole derivatives were designed following rational drug design, and synthesized through microwave-assisted one-pot multicomponent reactions. These compounds are produced in large quantities, and are known to be tolerant toward a variety of substrates, thus providing target molecules in a single step within a short time. These compounds were further tested for their ability to inhibit indoleamine-2,3-dioxygenase 1 (IDO1). The most promising compound thus obtained is 4o, which displayed IC₅₀ values of 0.82 μΜ. Further in vivo assessment indicated that 4o could reduce the kynurenine levels in plasma by 42.3% in 4 hr, indicating that the compound could act as a promising lead compound for further investigations.