Paper · 2026 · Pest Management Science

Design, synthesis, nematicidal activity, and preliminary mechanism of thiazole derivatives through the scaffold hopping strategy

Zongnan Zhu; Siyu Lu; Xiuhai Gan; et al.

11
claims
11
verbatim quotes
0
citations
1
research areas
—
Not open access

Abstract

Abstract BACKGROUND Plant‐parasitic nematodes (PPNs) pose a serious threat to global agricultural productivity. Most of the currently available nematicides have limitations in terms of efficacy and environmental safety. Therefore, there is an urgent need to discover new, highly effective and environmentally friendly nematicides. RESULTS A series of thiazole derivatives were designed and synthesized through a scaffold‐hopping strategy. Some of these compounds exhibited excellent nematicidal activity. Compound A1 displayed remarkable toxicity against Bursaphelenchus xylophilus , Aphelenchoides besseyi , and Meloidogyne incognita with median lethal concentration ( LC 50 ) values of 4.3, 1.9, and 6.2 mg/L, respectively, outperforming the commercial nematicide tioxazafen. Mechanistic studies revealed that compound A1 effectively inhibited nematode egg hatching, induced excessive accumulation of reactive oxygen species ( ROS ), and caused vacuolization in nematode tissues. Pot experiments demonstrated that compound A1 not only reduced nematode invasion but also enhanced the root defense response of tomato plants. Moreover, compound A1 significantly inhibited succinate dehydrogenase ( SDH ) activity in M. incognita , suggesting that interference with mitochondrial energy metabolism may contribute to its nematicidal effect. CONCLUSION Thiazole‐based compound A1 can serve as an excellent lead compound from which new nematicides can be discovered through structural optimization in the future. © 2026 Society of Chemical Industry.

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Claims 11

Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

Compound A1 was toxic to Bursaphelenchus xylophilus with an LC50 of 4.3 mg/L, outperforming the commercial nematicide tioxazafen.

Taxon
Bursaphelenchus xylophilusBursaphelenchus xylophiluse0
Treatment
Compound A1e0
Outcome
median lethal concentration ( LC 50 )e0
Direction
outperforminge0
Value
4.3e0
Comparator
tioxazafene0

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Bursaphelenchus xylophilus
Bursaphelenchus xylophilus · TaxonA. Steven Munson, USDA Forest Service, Bugwood.org · CC BY 3.0 us · Wikimedia Commons ↗

Verbatim

e0

“Compound A1 displayed remarkable toxicity against Bursaphelenchus xylophilus , Aphelenchoides besseyi , and Meloidogyne incognita with median lethal concentration ( LC 50 ) values of 4.3, 1.9, and 6.2 mg/L, respectively, outperforming the commercial nematicide tioxazafen”

✓ located verbatim in the source · abstract, characters 505–776 · show in text ↑
Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

Compound A1 was toxic to Aphelenchoides besseyi with an LC50 of 1.9 mg/L, outperforming the commercial nematicide tioxazafen.

Taxon
Aphelenchoides besseyiAphelenchoides besseyie0
Treatment
Compound A1e0
Outcome
median lethal concentration ( LC 50 )e0
Direction
outperforminge0
Value
1.9e0
Comparator
tioxazafene0

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Aphelenchoides besseyi
Aphelenchoides besseyi · TaxonDonald Groth, Louisiana State University AgCenter, Bugwood.org - See more at: http://www.forestryimages.org/browse/detail.cfm?imgnum=5390566#sthash.8Cvkh4nv.dpu · CC BY 3.0 · Wikimedia Commons ↗

Verbatim

e0

“Compound A1 displayed remarkable toxicity against Bursaphelenchus xylophilus , Aphelenchoides besseyi , and Meloidogyne incognita with median lethal concentration ( LC 50 ) values of 4.3, 1.9, and 6.2 mg/L, respectively, outperforming the commercial nematicide tioxazafen”

✓ located verbatim in the source · abstract, characters 505–776 · show in text ↑
Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

Compound A1 was toxic to Meloidogyne incognita with an LC50 of 6.2 mg/L, outperforming the commercial nematicide tioxazafen.

Taxon
Meloidogyne incognitaMeloidogyne incognitae0
Treatment
Compound A1e0
Outcome
median lethal concentration ( LC 50 )e0
Direction
outperforminge0
Value
6.2e0
Comparator
tioxazafene0

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Meloidogyne incognita
Meloidogyne incognita · TaxonPhoto by William Wergin and Richard Sayre. Colorized by Stephen Ausmus. U.S. Department of Agriculture · CC BY 2.0 · Wikimedia Commons ↗

Verbatim

e0

“Compound A1 displayed remarkable toxicity against Bursaphelenchus xylophilus , Aphelenchoides besseyi , and Meloidogyne incognita with median lethal concentration ( LC 50 ) values of 4.3, 1.9, and 6.2 mg/L, respectively, outperforming the commercial nematicide tioxazafen”

✓ located verbatim in the source · abstract, characters 505–776 · show in text ↑
Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

Compound A1 inhibited nematode egg hatching.

Taxon
nematodeNematodae0
Treatment
compound A1e0
Outcome
nematode egg hatchinge0
Direction
inhibitede0

Not reportedComparator

Verbatim

e0

“compound A1 effectively inhibited nematode egg hatching, induced excessive accumulation of reactive oxygen species ( ROS ), and caused vacuolization in nematode tissues”

✓ located verbatim in the source · abstract, characters 812–980 · show in text ↑
Intervention effectobservedoriginal resultmeasured

Claim · model-written summary

Compound A1 induced excessive accumulation of reactive oxygen species in nematodes.

Taxon
nematodeNematodae0
Treatment
compound A1e0
Outcome
accumulation of reactive oxygen species ( ROS )e0
Direction
excessivee0

Not reportedComparator

Verbatim

e0

“compound A1 effectively inhibited nematode egg hatching, induced excessive accumulation of reactive oxygen species ( ROS ), and caused vacuolization in nematode tissues”

✓ located verbatim in the source · abstract, characters 812–980 · show in text ↑
Intervention effectobservedoriginal resultmeasured

Claim · model-written summary

Compound A1 caused vacuolization in nematode tissues.

Taxon
nematodeNematodae0
Treatment
compound A1e0
Outcome
vacuolization in nematode tissuese0
Direction
causede0

Not reportedComparator

Verbatim

e0

“compound A1 effectively inhibited nematode egg hatching, induced excessive accumulation of reactive oxygen species ( ROS ), and caused vacuolization in nematode tissues”

✓ located verbatim in the source · abstract, characters 812–980 · show in text ↑
Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

In pot experiments, compound A1 reduced nematode invasion of tomato plants.

Treatment
compound A1e0
Interactor
nematodeNematodae0pest
Outcome
nematode invasione0
Direction
reducede0
Setting
Pot experimentse0

Not reportedComparator

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Solanum lycopersicum
Solanum lycopersicum · TaxonKod B · CC BY-SA 4.0 · Wikimedia Commons ↗

Verbatim

e0

“Pot experiments demonstrated that compound A1 not only reduced nematode invasion but also enhanced the root defense response of tomato plants”

✓ located verbatim in the source · abstract, characters 982–1123 · show in text ↑
Intervention effectobservedoriginal resultpositivemeasured

Claim · model-written summary

In pot experiments, compound A1 enhanced the root defense response of tomato plants.

Treatment
compound A1e0
Outcome
root defense responsee0
Direction
enhancede0
Setting
Pot experimentse0

Not reportedComparator

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Solanum lycopersicum
Solanum lycopersicum · TaxonKod B · CC BY-SA 4.0 · Wikimedia Commons ↗

Verbatim

e0

“Pot experiments demonstrated that compound A1 not only reduced nematode invasion but also enhanced the root defense response of tomato plants”

✓ located verbatim in the source · abstract, characters 982–1123 · show in text ↑
Intervention effectobservedoriginal resultpositivesignificant (as stated)measured

Claim · model-written summary

Compound A1 significantly inhibited succinate dehydrogenase activity in Meloidogyne incognita.

Taxon
M. incognitaMeloidogyne incognitae0
Treatment
compound A1e0
Outcome
succinate dehydrogenase ( SDH ) activitye0
Direction
inhibitede0

Not reportedComparator

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Meloidogyne incognita
Meloidogyne incognita · TaxonPhoto by William Wergin and Richard Sayre. Colorized by Stephen Ausmus. U.S. Department of Agriculture · CC BY 2.0 · Wikimedia Commons ↗

Verbatim

e0

“compound A1 significantly inhibited succinate dehydrogenase ( SDH ) activity in M. incognita”

✓ located verbatim in the source · abstract, characters 1135–1227 · show in text ↑
Mechanismhypothesisoriginal resultbasis n/a

Claim · model-written summary

The authors suggest that interference with mitochondrial energy metabolism may contribute to the nematicidal effect of compound A1 in M. incognita.

Taxon
M. incognitaMeloidogyne incognitae0
Outcome
nematicidal effecte0
Qualifier
interference with mitochondrial energy metabolisme0

Organisms pictured · Representative pictures of the matched species, not figures from the paper.

Meloidogyne incognita
Meloidogyne incognita · TaxonPhoto by William Wergin and Richard Sayre. Colorized by Stephen Ausmus. U.S. Department of Agriculture · CC BY 2.0 · Wikimedia Commons ↗

Verbatim

e0

“compound A1 significantly inhibited succinate dehydrogenase ( SDH ) activity in M. incognita , suggesting that interference with mitochondrial energy metabolism may contribute to its nematicidal effect”

✓ located verbatim in the source · abstract, characters 1135–1336 · show in text ↑
Recommendationauthor interpretationoriginal resultbasis n/a

Claim · model-written summary

Thiazole-based compound A1 can serve as a lead compound from which new nematicides can be discovered through structural optimization.

Outcome
lead compounde0

Not reportedTaxon

Verbatim

e0

“compound A1 can serve as an excellent lead compound from which new nematicides can be discovered through structural optimization”

✓ located verbatim in the source · abstract, characters 1364–1492 · show in text ↑