<p>Obesity is a complex health issue that has become a global pandemic due to its association with a range of diseases, including cardiovascular diseases, certain types of cancer, type 2 diabetes mellitus, chronic inflammation and high blood pressure. An extreme accumulation of fats in adipose tissue occurs when triacylglycerol (lipid) is broken down into mono-acyl glycerol and free fatty acids, which are then stored as energy in the adipose tissue. This can lead to severe obesity and dangerous human health issues. Accordingly, intensive research work was conducted in an effort to mitigate the problem of obesity and combat its consequences. Specifically, several research groups have carried out research work in search of synthetic anti-obesity drugs that are non-toxic, environmentally friendly, and can be produced from sustainable sources. Certain organic heterocyclic compounds containing hetero atom such as nitrogen, oxygen, and sulphur have demonstrated potential in combating obesity. In particular, quinazolinones, bis-indole derivatives, and di-spiroheterocycles are synthetic heterocyclic compounds that exhibit a wide range of biological activities such as anti-inflammatory effects, anti-obesity properties and the ability to lower lipid levels. These synthetic compounds, as well as specific natural heterocyclic compounds exhibit lipid inhibitory activity. Thus, this review article emphasizes the significance of both synthetic and natural heterocyclic compounds in combating obesity, along with various other biological activities.</p> Graphical abstract <p></p>