A protozoan infection called malaria is caused by Plasmodium parasites. In 2018, it infected more than 228 million people and caused 405,000 fatalities. Worryingly, the present antimalarial drugs had developed drug resistance. Furthermore, they are associated with adverse effects and price issues. Amidst the gloomy scenario, drug discovery based on natural products had renewed the hope to overcome the burdens associated with the present antimalarial drugs. Auspiciously, medicinal plants had contributed significantly to the modern pharmacotherapy of malaria. Interestingly, Acacia pennata (L.) Willd. was also documented as a traditional antimalarial agent. However, there is still no scientific evidence regarding its antimalarial activity. Therefore, this article was aimed to study the phytochemical profile of A. pennata and explore their potential activity against malarial parasites. A. pennata contains different classes of bioactive compounds such as alkaloids, flavonoids, phenols, glycosides, terpenoids, phytosterols, and saponins whose antimalarial activities had been reported. Accordingly, the future scopes and challenges regarding the possible antimalarial activity for A. pennata are also discussed. To maximize the chances for finding a new antimalarial chemical entity from A. pennata, a schematic flow chart on the ethnopharmacology based drug discovery approach is also provided. Thus, this literary work may be used by researchers as a referential guide in the search for new antimalarial phytochemicals.