Biotic stresses (fungi, bacteria, insects, weeds, etc.) are some of the most important causes of the decrease in thequality and quantity of crops that could become an emergency due to a noteworthy increase in the world population. Thus, toovercome these problems, massive use of chemical pesticides has been carried out with heavy consequences for environmentalpollution and food safety. An eco-friendly alternative can be using natural compound-based biopesticides with high efficacy andselectivity. Some bacterial lipodepsipeptides (tolaasins I, II, A, D, and E and WLIP together with hexacetyl- and tetrahydro-tolaasin Iand 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 growthinhibition of all microorganisms tested in the range of 0.1-0.8 mu g/mL, while cyclodipeptides, despite preserving this ability, showeda noteworthily reduced antimicrobial activity being active only in the range of 15-900 mu g/mL. Among the lipodepsipeptides andcyclic dipeptides assayed, tolaasinDand 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 biopesticidesin agriculture.