The biological potential of various heterocyclic scaffolds draw special attention of medicinal chemists and hence exhaustive efforts are being carried out in the search of lead molecules pertaining to it. The knowledge of such biologically important heterocycles and their methods of synthesis are discussed in this review. Especially, the focus is kept on the heterocycles that are effective to treat many significant lifestyle diseases such as atherosclerosis, diabetes, ischemic heart disease, myocardial infarctions, which are strongly associated with imbalance in lipid metabolism and plasma lipoproteins. As these conditions are responsible for one-third of deaths in industrialized nations, special emphasis is given on synthesis of recently reported heterocycles possessing anti-hyperlipidemic activity. Such derivatives have been extensively studied in the past few decades. The present review includes the rigorous literature survey on the methods of preparation along with the potential biological activities correcting lipid metabolism.