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LEAD:
A lead compound (i.e. a "leading" compound)
with various compounds of the metallic element
lead) in drug discovery is a chemical compound
that has pharmacological or biological activity
likely to be therapeutically useful, but may
nevertheless have suboptimal structure that
requires modification to fit better to the target
Development of a lead compound:
A lead compound may arise from a variety of
different sources. Lead compounds are found by
characterizing natural products, employing
combinatorial chemistry, or by molecular
modeling as in rational drug design. Chemicals
identified as hits through high-throughput
screening may also become lead compounds.
Once a lead compound is selected it must undergo
lead optimization, which involves making the
compound more "drug-like.
Lead compounds with their sources and
clinical uses:
Lead
compounds
Clinical use sources
Acetyldigoxin Cardiotonic Digitalis
lanata
Adoniside Cardiotonic Adonis
venmalis
Betulinic acid anticancer Betula alba
Caffeine CNS stimulant Camellia
sinensis
Codeine Analgesic P.somniferum
Etoposide Antitumer Podophyllum
peltatum
Glycyrrhizin Addison`s
disease
Glycyrrhyza
glabra
Morphine Analgesic P.somniferum
Nicotin Insecticide N.tabacum
Papain Proteolytic Carica
papaya
Quinine Antimalarial Cinchona
ledgeriana
……etc
.
Discovery of LEAD compounds from
plants
.
LEAD COMPOUNDS FROM NATURAL PRODUCT
KRISHNA PRIYA JHA, HARISH SHARMA
DEPARTMENT OF PHARMACY
ASHOKA INSTITUTE OF TECHNOLOGY AND MANAGEMENT VARANASI
NATIONAL CONFRRENCE
ORGANISED BY-
GOEL INSTITUTE OF PHARMACY AND SCIENCES, LUCKNOW