Pipermoola (Piper longum root) can be therapeutically valuable and useful as a nutraceutical due to various chemical components, primarily pseudoalkaloids and alkamides. In the Indian system of medicine, it is used in colds, asthma, and arthritis. It is used for improving decongestion, antibiotics, analgesic effects, rheumatism, epilepsy, indigestion, and gynecological diseases. Pipalli is reportedly part of more than 135 classical Ayurvedic formulations and one of the most used medicinal plants. Piper has gained attention for its wide range of pharmacological benefits and bioenhancer properties of piperine found in the fruit. The present chapter explores the underutilized parts of P. longum, i.e., root, as a sustainable bioactive source, particularly pseudoalkaloids and alkamides. Alkamides are a broad and expanding group of bioactive naturals that mostly contain a polyunsaturated aliphatic fatty acid chain with a shorter substituent of amine components and are linked together with different unsaturated fatty acids via a polypeptides amide linkage as observed in proteins. The pancreatic lipase inhibitory properties of Piper bioactive could be transilience in combating obesity. Various lipase inhibitors are discussed for their potential as a natural and sustainable alternative for pharmaceutical purposes. Piper compounds with lipase inhibitory potential could be crucial in preventing the hydrolysis of dietary fats into absorbable free fatty acids and monoacylglycerols. Piper longum, with its abundance of bioactive pseudoalkaloids, presents a promising avenue for developing antiobesity agents.