Designing Trifluoromethyl Pyrazolones for Selective Molluscicidal Activity Against <i>Monacha cartusiana</i>: Toward Sustainable Land Snail Control

Terrestrial gastropods are significant agricultural pests and disease carriers, posing major challenges to farm crops and various agricultural domains. Synthetic pesticides remain the primary method of pest control, but rising resistance and harmful effects on nontarget species highlight the urgent need for new, safer alternatives. Herrin, we report on the synthesis and the evaluation of a series of 5-trifluoromethyl-phenylpyrazolones against <i>Monacha cartusiana</i> (O. F. Müller, 1774) snails as potential molluscicidal agents. The newly synthesized 5-trifluoromethyl-phenyl pyrazolones derivatives <b>11-24</b> were characterized based on <sup>1</sup>H NMR, <sup>13</sup>C-APT and <sup>19</sup>F- NMR spectra as well as mass spectroscopy. Compounds <b>11</b>, <b>16</b>, <b>17</b> and <b>18</b> demonstrated potent anti-<i>M. cartusiana</i> activities, with <b>16</b> exhibiting the highest lethal activity (LC<sub>50</sub> = 0.58 mg/mL), surpassing the current standard, methomyl (LC<sub>50</sub> = 2.28 mg/mL). Significant increase in liver transaminase enzymes (AST and ALT), acetylcholinesterase (AChE), along with reduction in total carbohydrates and lipids, were observed after the treatment of <i>M. cartusiana</i> snails with compounds <b>11</b>, <b>16</b>, <b>17</b>, and <b>18</b> at the LC<sub>50</sub> values. Histopathological analysis of the digestive glands of treated snails revealed induced cellular damage, with the greatest structural cellular integrity loss and functional impairment observed for compound <b>16</b>. Additionally, typical CNS toxicity symptoms, including paralysis and excessive fluid secretion, suggest a dual mode of action: gastrointestinal toxicity and GABA<sub>A</sub>-glutamate chloride ion channel (GluCl) antagonism. Homology modeling using the 3RHW (<i>Caenorhabditis elegans</i> (Maupas, 1900)) template and a GluCl ζ-subunit sequence were used to generate a 3RHW- ζ chimera for virtual screening. Additionally, induced fit docking (IFD) studies using GABA<sub>A</sub> GluCl structures were used to generate trifluoromethylphenylpyrazole-compatible binding pockets. Docking scores derived from these models were found to support the observed molluscicidal activity. These findings identified potent 4-substituted-5-trifluoromethylphenylpyrazolones as potential useful candidates for safer, effective molluscicides.

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Journal
Journal of Agricultural and Food Chemistry
Published
2025-06-11
DOI
https://doi.org/10.1021/acs.jafc.4c12327
Primary Topic
Insect and Pesticide Research
Type
article
Field-Weighted Citation Impact
0.00

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article

Designing Trifluoromethyl Pyrazolones for Selective Molluscicidal Activity Against Monacha cartusiana: Toward Sustainable Land Snail Control

F. El-Akhrasy, Reham A. I. Abou‐Elkhair, Abdalla E. A. Hassan, Yasir S. Raouf et al.
Journal of Agricultural and Food Chemistry
Insect and Pesticide Research
article

Designing Trifluoromethyl Pyrazolones for Selective Molluscicidal Activity Against Monacha cartusiana: Toward Sustainable Land Snail Control

F. El-Akhrasy, Reham A. I. Abou‐Elkhair, Abdalla E. A. Hassan, Yasir S. Raouf, Shaikha S. AlNeyadi, Hend M. Maaroof
article en

Abstract

Terrestrial gastropods are significant agricultural pests and disease carriers, posing major challenges to farm crops and various agricultural domains. Synthetic pesticides remain the primary method of pest control, but rising resistance and harmful effects on nontarget species highlight the urgent need for new, safer alternatives. Herrin, we report on the synthesis and the evaluation of a series of 5-trifluoromethyl-phenylpyrazolones against <i>Monacha cartusiana</i> (O. F. Müller, 1774) snails as potential molluscicidal agents. The newly synthesized 5-trifluoromethyl-phenyl pyrazolones derivatives <b>11-24</b> were characterized based on <sup>1</sup>H NMR, <sup>13</sup>C-APT and <sup>19</sup>F- NMR spectra as well as mass spectroscopy. Compounds <b>11</b>, <b>16</b>, <b>17</b> and <b>18</b> demonstrated potent anti-<i>M. cartusiana</i> activities, with <b>16</b> exhibiting the highest lethal activity (LC<sub>50</sub> = 0.58 mg/mL), surpassing the current standard, methomyl (LC<sub>50</sub> = 2.28 mg/mL). Significant increase in liver transaminase enzymes (AST and ALT), acetylcholinesterase (AChE), along with reduction in total carbohydrates and lipids, were observed after the treatment of <i>M. cartusiana</i> snails with compounds <b>11</b>, <b>16</b>, <b>17</b>, and <b>18</b> at the LC<sub>50</sub> values. Histopathological analysis of the digestive glands of treated snails revealed induced cellular damage, with the greatest structural cellular integrity loss and functional impairment observed for compound <b>16</b>. Additionally, typical CNS toxicity symptoms, including paralysis and excessive fluid secretion, suggest a dual mode of action: gastrointestinal toxicity and GABA<sub>A</sub>-glutamate chloride ion channel (GluCl) antagonism. Homology modeling using the 3RHW (<i>Caenorhabditis elegans</i> (Maupas, 1900)) template and a GluCl ζ-subunit sequence were used to generate a 3RHW- ζ chimera for virtual screening. Additionally, induced fit docking (IFD) studies using GABA<sub>A</sub> GluCl structures were used to generate trifluoromethylphenylpyrazole-compatible binding pockets. Docking scores derived from these models were found to support the observed molluscicidal activity. These findings identified potent 4-substituted-5-trifluoromethylphenylpyrazolones as potential useful candidates for safer, effective molluscicides.

Journal of Agricultural and Food ChemistryVol. 73(32)
Zagazig University (EG), United Arab Emirates University (AE), Environment and Plant Protection Research Institute (CN), Bridge Of Nucleic Acids Chemistry (Japan) (JP), Agricultural Research Center (EG)
College of Graduate Studies, United Arab Emirates University
Openalex Percentile: Top 88%
Insect and Pesticide Research
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