Anthranilic acid is a benzenoid compound that has adjacent active important two reactive groups namely carboxylic acid group (-COOH) and amino group (-NH2). Consequently fascinating anthranilic acid derivatives have been prepared through both the active functional groups. The literature review reveals an experiential and holistic approach of various manufacturing procedures and skills used for the production of anthranilic acid analogues and anthranilic scaffold along with the biological activities of some of the promising derived anthranilic acid molecules. Pharmacology of anthranilic acid derivatives has been reported as alpha-glucosidase inhibitors, urease suppressors, keto-aldo reductase undecaprenyl pyrophosphate synthase (UppS) suppressors, mitogen activated protein kinase (MAPK), COX(Cyclooxygenase) inhibitors The analogues of anthranilic acid have been reported as an excellent pharmaceutical aids such as anticancer, antidiabetic, antiviral, anti-inflammatory, analgesic and antimicrobial agents. The present review unveils the importance of anthranilic scaffold as a beginning material for the development of potent drug for their various pharmacological activities.