Executive Summary : | Natural products and it’s non-natural analogues show diverse biological activities and hence are studied extensively in several research and development centers in pharmaceutical industry and in medicinal chemistry programs. One of the key concerns in direct application of natural product targets as drug molecules is their limited availability. Secondly, their existing physicochemical properties need fine tuning that is necessary for drug metabolism as per Lipinski’s rule of 5. Synthetic organic chemists often address this concern by having efficient processes which provide more amounts of the target compounds and its analogues. This strategy of using diketopiperazinone core with acridones and β-lactams is not known in literature and is aimed to provide newer molecules that would serve as promising pharmaceutical leads. Diketopiperazine motif is widely studied and also found in several natural products. They have been found to exhibit interesting biological activities anti-cancer, anti-viral, anti-oxidant etc. Although there has been lot of interest in diketopiperazine synthesis, a focused dual approach/design for synthesis of ketopiperazine-based fused heterocycles along with natural amino acid incorporation is not well precedented. Acridines such as Amsacrine are known anti-cancer drugs in market that work by inhibition of Topoisomerase-II enzyme. The strategy is aimed to provide an easy access to related molecules that can be screened for biological activities. Several acridones and acridine based natural products are known to be showing good anti-cancer properties. Secondly, the β-lactam based piperazinone core would serve as novel molecules as anti-bacterial agents. More importantly, the proposed strategy employs metal-free sustainable chemistry approaches and use of natural amino-acids which are present in biological systems and thus the resulting compounds and cyclopeptides would have good scope for further exploitation as promising leads. |