Plant-endophyte associations represent an inexhaustible source of novel metabolites, exhibiting
significance in environment, agriculture and pharmaceutical perspectives. The global outbreak
of life-threatening diseases necessitates a need for a more targeted approach through efficient
drug-discovery programs. In recent times, endophytes as “bio-factories” have been extensively explored
for the production of novel bioactive metabolites demonstrating therapeutic properties. Resources
in computational biology co-integrated with combinational chemistry have made significant
contributions in this field, aiding in discovery and screening of potential “drug-like”
molecules from endophytes. The review provides a meta-analysis of bioactive metabolite production
from endophytes, extensively discussing the bio-prospection of natural products for pharmaceutical
applications. In light of emerging importance of endophytes as anti-infective agents, an exploration
of the pharmaceutical design of novel chemical entities and analogues has enabled efficient
and cost-effective drug discovery programs. However, bottlenecks in endophyte biology and
research require a better understanding of endophyte dynamics and mechanism of bioactive metabolite
production towards a sustainable drug discovery program.
Keywords: Anti-infective, Bioactive, Bio-prospection, Drug discovery, Endophytes, Natural products, Pharmaceutical design.
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