14385-65-0Relevant academic research and scientific papers
Novel 4,5-dihydro-1H-pyrazole derivatives as potential succinate dehydrogenase inhibitors: design, synthesis, crystal structure, biological activity and molecular modeling
Zhang, Tingting,Liu, Hui,Lu, Tong,Zhang, Guilan,Xiao, Tingting,Cheng, Wei,Wang, Jingwen,Jiang, Wenjing,Tang, Xiaorong
, (2021/10/05)
Twenty-eight new 4, 5-dihydro-1H-pyrazole derivatives were designed, synthesized and characterized by IR, 1H NMR, 13C NMR and HRMS. The crystal structure of compound 2j was characterized by single crystal X-ray diffraction. Their ant
Design, synthesis, and antifungal activity evaluation of novel 2-cyano-5-oxopentanoic acid derivatives as potential succinate dehydrogenase inhibitors
Mai, Yong-zhan,Peng, Mi-jun,Tang, Xiao-rong,Wang, Xue-song
, p. 94 - 107 (2021/11/22)
Two series of novel 2-cyano-5-oxopentanoic acid derivatives (1a?l, 2a?l) were designed, synthesized, and characterized by IR, 1H NMR, 13C NMR, and HRMS. Their in vitro antifungal activity against five plant pathogenic fungi were then
Design, synthesis and insecticidal activity of novel semicarbazones and thiosemicarbazones derived from chalcone
Cheng, Wei,Xiao, Tingting,Qian, Weifeng,Lu, Tong,Zhang, Tingting,Tang, Xiaorong
, p. 3801 - 3809 (2020/03/23)
Thirty semicarbazone and thiosemicarbazone derivatives (2a–w and 4a–g) from chalcones containing furan and thiophene ring were designed and synthesized. They were characterized by IR, 1H NMR, 13C NMR and HRMS. The crystal structure o
2-(4-chlorphenyl) pyridine compound and application thereof in pesticide
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Paragraph 0064-0066, (2021/06/13)
The invention relates to a 2-(4-chlorphenyl) pyridine compound and application thereof in pesticides, and belongs to the technical field of pesticides. The structural formula of the 2-(4-chlorphenyl) pyridine compound is as shown in formula (I), in the fo
2, 3, 4, 6-tetrasubstituted pyridine compound and application thereof in pesticides
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Paragraph 0064-0066, (2021/06/22)
The invention relates to a 2, 3, 4, 6-tetrasubstituted pyridine compound and application thereof in pesticides, which belong to the technical field of pesticides. The structural formula of the 2, 3, 4, 6-tetrasubstituted pyridine compound disclosed by the
Novel potent and selective DPP-4 inhibitors: Design, synthesis and molecular docking study of dihydropyrimidine phthalimide hybrids
Mourad, Ahmed A. E.,Khodir, Ahmed E.,Saber, Sameh,Mourad, Mai A. E.
, p. 1 - 24 (2021/02/26)
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as antihyperglycemic agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in combination with other antidiabetic drugs. Methods: A novel series of dihydropyrimidine phthalimide hybrids was synthesized and evaluated for their in vitro and in vivo DPP-4 inhibition activity and selectivity using alogliptin as reference. Oral glucose tolerance test was assessed in type 2 diabetic rats after chronic treatment with the synthesized hybrids ± metformin. Cytotoxicity and antioxidant assays were performed. Additionally, molecular docking study with DPP-4 and structure activity relationship of the novel hybrids were also studied. Results: Among the synthesized hybrids, 10g, 10i, 10e, 10d and 10b had stronger in vitro DPP-4 inhibitory activity than alogliptin. Moreover, an in vivo DPP-4 inhibition assay revealed that 10g and 10i have the strongest and the most extended blood DPP-4 inhibitory activity compared to alogliptin. In type 2 diabetic rats, hybrids 10g, 10i and 10e exhibited better glycemic control than alogliptin, an effect that further supported by metformin combination. Finally, 10j, 10e, 10h and 10d had the highest radical scavenging activity in DPPH assay. Conclusions: Hybrids 10g, 10i and 10e are potent DPP-4 inhibitors which may be beneficial for T2DM treatment.
3-(4-chlorphenyl)-4, 5-dihydropyrazole derivative and application thereof in pesticides
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Paragraph 0055-0057, (2020/04/17)
The invention relates to a 3-(4-chlorphenyl)-4, 5-dihydropyrazole derivative and an application thereof in pesticides, and belongs to the technical field of pesticides. The technical problem to be solved by the invention is to provide a novel compound which can be used as an agricultural bactericide and a seed germination accelerator. The structural formula of the compound is shown in the formulaI, wherein X is oxygen, sulfur or nitrogen and R is hydrogen, methyl, methoxyl, hydroxymethyl, chlorine or bromine. The compound has good inhibitory activity on plant pathogenic fungi, has a good promotion effect on germination of vegetable seeds and lays a good foundation for creation of new pesticides.
Studies of NMR Chemical Shifts of Chalcone Derivatives of Five-membered Monoheterocycles and Determination of Aromaticity Indices
Jeong, Eun Jeong,Lee, In-Sook Han
, p. 668 - 673 (2019/07/12)
A series of the chalcone derivatives of the five-membered monoheterocyclic compounds, (E)-1-aryl-3-heteroarylpropen-1-ones, were prepared by aldol condensation of the corresponding aldehydes of thiophene, pyrrole, and furan with m- and p-substituted acetophenones. Similar condensation of the acetyl compounds of the heterocycles with m- and p-substituted benzaldehydes gave another series of the chalcone derivatives, (E)-1-heteroaryl-3-arylpropen-1-ones. The 13C chemical shift values (δC) of the chalcone derivatives were determined in order to find if they correlated with the Hammett σ values. A good correlation, especially for the β-C for both series, was found for the 13C chemical shift values (δC) of the chalcone derivatives with the Hammett σ values. The chemical shift values of the β-C of the heterocyclic compounds were plotted against those of the benzene derivatives. The resulting slopes were found to be close to the values of the aromaticity indices.
N1-benzenesulfonyl-2-pyrazoline hybrids in neurological disorders: Syntheses, biological screening and computational studies
Tripathi, Avinash C.,Upadhyay, Savita,Paliwal, Sarvesh,Saraf, Shailendra K.
, p. 126 - 148 (2018/02/14)
A novel series of 1,3,5-trisubstituted-2-pyrazolines (5a-5t) was prepared via Claisen Schmidt condensation, followed by heterocyclization with hydrazine hydrate, substitution of N1 hydrogen of 2-pyrazoline nucleus with 4-chlorobenzenesulfonylchloride, app
Derivatives of 4,5-dihydro (1H) pyrazoles as possible MAO-A inhibitors in depression and anxiety disorders: synthesis, biological evaluation and molecular modeling studies
Tripathi, Avinash C.,Upadhyay, Savita,Paliwal, Sarvesh,Saraf, Shailendra K.
, p. 1485 - 1503 (2018/03/29)
A series of 1,3,5-trisubstituted-2-pyrazoline derivatives (3a–3t) were synthesized in appreciable yields by substituting N1 position of 2-pyrazoline nucleus with 4-nitrobenzenesulfonylchloride using conventional and microwave assisted synthetic approaches
