Natural product chemistry is an important class of organic chemistry that
contributes novel organic compounds to the chemical literature and is considered as
one of the successful sources of supplying lead bioactive compounds to the drug
discovery. One of the aspects of drug discovery is the identification of small molecules
with enzyme inhibiting activities. Enzymes play an important role in all aspects of
health in life and their overexpression and hyperactivation is involved in the
pathogenesis of various diseases. For instance, anti-acetylcholinesterase (AChE)
compounds are potential candidates for curing Alzheimer’s Disease (AD). During the
past years, we are involved in discovering new enzyme inhibiting natural products from
medicinally important plants. This chapter describes the identification of new anti-α-
glucosidase, anti-renin, anti-glutathione transferase (GST) and anti-AChE compounds
from medicinally important plants. Additionally, structure-activity relationships (SAR)
and determination of active pharmacophores of newly discovered bioactive natural
products exhibiting aforementioned bioactivities are also discussed.
Keywords: Alzheimer’s Disease, α-glucosidase, Glutathione Transferase (GST),
Acetylcholinesterase, Natural Products, Diabetes, Hypertension, Chemoenzymatic
Synthesis.
