دورية أكاديمية

Discovery of Novel Pyrazole Acyl Thiourea Skeleton Analogue as Potential Herbicide Candidates.

التفاصيل البيبلوغرافية
العنوان: Discovery of Novel Pyrazole Acyl Thiourea Skeleton Analogue as Potential Herbicide Candidates.
المؤلفون: Ma C; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Tian L; Bohai College, Hebei Agricultural University, Baoding 071001, P. R. China., Wang YE; College of Science, Hebei Agricultural University, Baoding 071001, P. R. China., Huo J; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., An Z; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Sun S; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Kou S; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Wang W; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Li Y; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Zhang J; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China., Chen L; College of Plant Protection, Hebei Agricultural University, Baoding 071001, P. R. China.
المصدر: Journal of agricultural and food chemistry [J Agric Food Chem] 2024 Apr 10; Vol. 72 (14), pp. 7727-7734. Date of Electronic Publication: 2024 Mar 26.
نوع المنشور: Journal Article
اللغة: English
بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 0374755 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-5118 (Electronic) Linking ISSN: 00218561 NLM ISO Abbreviation: J Agric Food Chem Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Washington, American Chemical Society.
مواضيع طبية MeSH: Herbicides*/pharmacology , Herbicides*/chemistry , Cyclohexanones* , Pyridines* , Sulfonylurea Compounds*, Structure-Activity Relationship ; Molecular Docking Simulation ; Skeleton ; Pyrazoles/pharmacology ; Pyrazoles/chemistry ; Thiourea
مستخلص: To discover novel transketolase (TKL, EC 2.2.1.1) inhibitors with potential herbicidal applications, a series of pyrazole acyl thiourea derivatives were designed based on a previously obtained pyrazolamide acyl lead compound, employing a scaffold hopping strategy. The compounds were synthesized, their structures were characterized, and they were evaluated for herbicidal activities. The results indicate that 7a exhibited exceptional herbicidal activity against Digitaria sanguinalis and Amaranthus retroflexus at a dosage of 90 g ai/ha, using the foliar spray method in a greenhouse. This performance is comparable to that of commercial products, such as nicosulfuron and mesotrione. Moreover, 7a showed moderate growth inhibitory activity against the young root and stem of A. retroflexus at 200 mg/L in the small cup method, similar to that of nicosulfuron and mesotrione. Subsequent mode-of-action verification experiments revealed that 7a and 7e inhibited Setaria viridis TKL ( Sv TKL) enzyme activity, with IC 50 values of 0.740 and 0.474 mg/L, respectively. Furthermore, they exhibited inhibitory effects on the Brassica napus acetohydroxyacid synthase enzyme activity. Molecular docking predicted potential interactions between these ( 7a and 7e ) and Sv TKL. A greenhouse experiment demonstrated that 7a exhibited favorable crop safety at 150 g ai/ha. Therefore, 7a is a promising herbicidal candidate that is worthy of further development.
فهرسة مساهمة: Keywords: acetohydroxyacid synthase; acyl thiourea; herbicidal activity; transketolase
المشرفين على المادة: 0 (Herbicides)
CG297D9264 (nicosulfuron)
48TR68G21T (mesotrione)
0 (Pyrazoles)
GYV9AM2QAG (Thiourea)
0 (Cyclohexanones)
0 (Pyridines)
0 (Sulfonylurea Compounds)
تواريخ الأحداث: Date Created: 20240326 Date Completed: 20240411 Latest Revision: 20240411
رمز التحديث: 20240411
DOI: 10.1021/acs.jafc.3c08863
PMID: 38530940
قاعدة البيانات: MEDLINE
الوصف
تدمد:1520-5118
DOI:10.1021/acs.jafc.3c08863