Polycystic Ovarian Syndrome (PCOS) is the most prevalent hormonal disorder that affects metabolism, ovulation and menstrual cycles. SIRT1 belongs to the Sirtuin family, a group of NAD+ dependent class 3 histone deacetylases. This review explores the correlation between SIRT1 and PCOS and associated mechanisms of action like Insulin resistance, oxidative stress, inflammation and autophagy. Extensive studies have been done on SIRT1, how it was downregulated and contributed to conditions like insulin resistance. How activation of SIRT1 helps by deacetylating the different responsible transcriptional factors is discussed in the mechanisms briefly. Additionally, we discussed the molecular structures of the existing natural and synthetic SIRT1 activators and their roles, which were previously reported, from the chemistry perspective. This review gives insights into the challenges and advantages of SIRT1, which can be a beneficial therapeutic target for PCOS.