Biotic stresses (fungi,
bacteria, insects, weeds, etc.) are some
of the most important causes of the decrease in the quality and quantity
of crops that could become an emergency due to a noteworthy increase
in the world population. Thus, to overcome these problems, massive
use of chemical pesticides has been carried out with heavy consequences
for environmental pollution and food safety. An eco-friendly alternative
can be using natural compound-based biopesticides with high efficacy
and selectivity. Some bacterial lipodepsipeptides (tolaasins I, II,
A, D, and E and WLIP together with hexacetyl- and tetrahydro-tolaasin
I and WLIP methyl ester) and cyclic dipeptides (cyclo(
l
-Pro-
l
-Tyr), cyclo(
d
-Pro-
l
-Tyr), cyclo(
l
-Pro-
l
-Val), and cyclo(
l
-Pro-
l
-Leu)) were
assayed against several pathogenic bacteria and fungi of important
agrarian plants. Lipodepsipeptides showed strong growth inhibition
of all microorganisms tested in the range of 0.1–0.8 μg/mL,
while cyclodipeptides, despite preserving this ability, showed a noteworthily
reduced antimicrobial activity being active only in the range of 15–900
μg/mL. Among the lipodepsipeptides and cyclic dipeptides assayed,
tolaasin
d
and cyclo(
l
-Pro-
l
-Tyr) (also
named maculosin-1) appeared to be the most toxic compounds. Some structure–activity
relationships of lipodepsipeptides were also discussed along with
their practical application as biopesticides in agriculture.