In modern agriculture and weed management
practices, herbicides
have been widely used to control weeds effectively and represent more
than 50% of commercial pesticides applied in the world. Herbicides
with unique mechanisms of actions (MOA) have historically been discovered
and commercialized every two or three years from the 1950s to the
1980s. However, this trend lowered dramatically as no herbicide with
a novel MOA has been marketed for more than 30 years. The fast-growing
resistance to commercial herbicides has reignited the agricultural
chemical industry interest in new structural scaffolds targeting novel
sites in plants. Carbon–phosphorus bonds (C–P) containing
natural products (NPs) have played an essential role in herbicide
discovery as the chemical diversity, and the promising bioactivity
of natural C–P phytotoxins can provide exciting opportunities
for the discovery of both natural and semisynthetic herbicides with
novel targets. Among commercial herbicides, glyphosate (Roundup),
a famous C–P containing herbicide, is by far the most universally
used herbicide worldwide. Furthermore, glufosinate is one of the most
widely used natural herbicides in the world. Therefore, C–P
NPs are a treasure for discovering new herbicides with novel mechanisms
of actions (MOAs). Here, we present an overview of the chemistry and
biology of glufosinate including isolation and characterization, mode
of action, herbicidal use, biosynthesis, and chemical synthesis since
its discovery in order to not only help scientists reassess the role
of this famous herbicide in the field of agrichemical chemistry but
also build a new stage for discovering novel C–P herbicides
with new MOAs.