Bryophytes and pteridophytes have been very communal among the tribal people in various parts of the world since time immemorial and have been evidenced to be useful in various grounds like food, tea, and medicines. Improvement in technologies in the human health sector has supported the inspections of the significant functional activities of these groups of plants, which have in turn dilated the scope of using these groups of neglected plants as a great boon for the pharmaceutical companies and their akin divisions. Different systems of medicines like Ayurvedic, homeopathic, and Unani have fruitfully utilized the therapeutic properties of fern and their allies in their system of medicines, after the in vitro screening of the latter. Dipteris wallichii (R.Br.) T. Moore, an endemic fern of the northeastern region of India, is considered one of the rare genera with very few records available, concerning its phytochemical and ethnomedicinal importance. The rhizome of this species is recorded to be useful as a hepatoprotective agent. Very delimited distribution and lack of easy approachability to this plant permits it to be called an endangered species, which has in turn called upon to study the chemical and molecular characterization including the pharmacological evaluation of this particular plant that is anticipated to hold high probabilities to be used as drugs in the medical world. In this chapter, bioactive compounds isolated from D. wallichii have been discussed, which are shown to have high therapeutic efficacy. Among these compounds, an alkaloid has been reported to be one of the most promising inhibitors against the human β secretase enzyme, a potent and highly anticipated drug target for Alzheimer’s disease. In addition to pondering upon the necessary conservatory measures to save this hidden treasure, there is a lot more to explore about the biological activity of the chemical compounds found in this interesting plant before it gets completely extinct. © 2023, Springer Nature Switzerland AG.