Design, Synthesis, and Herbicidal Activity of Thioether Containing 1,2,4-Triazole Schiff Bases as Transketolase Inhibitors

2021 ◽  
Author(s):  
Yan-En Wang ◽  
Dongchen Yang ◽  
Jingqian Huo ◽  
Lai Chen ◽  
Zhanhai Kang ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Herbicidal Activity ◽  
Design Synthesis

scholarly journals Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2593 ◽  
Author(s):  
Ashraf S. Hassan ◽  
Ahmed A. Askar ◽  
Ahmed M. Naglah ◽  
Abdulrahman A. Almehizia ◽  
Ahmed Ragab
Keyword(s):  
Molecular Docking ◽  
Schiff Bases ◽  
Dihydrofolate Reductase ◽  
Enzyme Assay ◽  
Dna Gyrase ◽  
Docking Study ◽  
Biological Evaluation ◽  
Immunomodulatory Activity ◽  
Molecular Docking Study ◽  
Design Synthesis

A series of Bis-pyrazole Schiff bases (6a–d and 7a–d) and mono-pyrazole Schiff bases (8a–d and 9a–d) were designed and synthesized through the reaction of 5-aminopyrazoles 1a–d with aldehydes 2–5 using mild reaction condition with a good yield percentage. The chemical structure of newly formed Schiff bases tethered pyrazole core was confirmed based on spectral and experimental data. All the newly formed pyrazole Schiff bases were evaluated against eight pathogens (Gram-positive, Gram-negative, and fungi). The result exhibited that, most of them have good and broad activities. Among those, only six Schiff bases (6b, 7b, 7c, 8a, 8d, and 9b) displayed MIC values (0.97–62.5 µg/mL) compared to Tetracycline (15.62–62.5 µg/mL) and Amphotericin B (15.62–31.25 µg/mL), MBC values (1.94–87.5 µg/mL) and selectivity to tumor cell than normal cells. Immunomodulatory activities showed that the promising Schiff bases increase the immunomodulator effect of defense cell and the Schiff base 8a is the highest one by (Intra. killing activity = 136.5 ± 0.3%) having a pyrazole moiety as well as amide function (O=C-NH2) and piperidinyl core. Furthermore, the most potent one exhibited broad activity depending on both MIC and MBC values. Moreover, to study the mechanism of these pyrazole Schiff bases, two active Schiff bases 8a and 9b from six derivatives were introduced to study the enzyme assay as dihydrofolate reductase (DHFR) on E. coli organism and DNA gyrase with two different organisms, S. aureus and B. subtilis, to determine the inhibitory activities with lower values in the case of DNA gyrase (8a and 9b) or nearly as DHFR compound 9b, while pyrazole 8a showed excellent inhibitory against all enzyme assay. The molecular docking study against dihydrofolate reductase and DNA gyrase were performed to study the binding between active site in the pocket with the two Schiff bases (8a and 9b) that exhibited good binding affinity with different bond types as H-bonding, aren-aren, and arene-cation interaction as well as study the physicochemical and pharmacokinetic properties of the two active Schiff bases 8a and 9b.

Design, Synthesis, and Herbicidal Activity of N-Benzyl-5-cyclopropyl-isoxazole-4-carboxamides

2020 ◽  
Vol 68 (51) ◽  
pp. 15107-15114
Author(s):  
Xin-Lin Sun ◽  
Zhen-Meng Ji ◽  
Shao-Peng Wei ◽  
Zhi-Qin Ji
Keyword(s):  
Herbicidal Activity ◽  
Design Synthesis

scholarly journals Design, synthesis, and herbicidal activity of sec-p-menthane-7-amine derivatives as botanical herbicides

RSC Advances ◽  
2021 ◽  
Vol 11 (44) ◽  
pp. 27207-27214
Author(s):  
Hongmei Zhang ◽  
Yuxiang Chen ◽  
Shichao Xu ◽  
Jing Wang ◽  
Huanhuan Dong ◽  
...  
Keyword(s):  
Herbicidal Activity ◽  
Design Synthesis ◽  
Barnyard Grass

In this study, a series of novel sec-p-menthane-7-amine derivatives were designed, synthesized, and evaluated to be used as efficient botanical herbicides owing to their post-emergence herbicidal activities against barnyard grass and rape.

Novel phenoxy-(trifluoromethyl)pyridine-2-pyrrolidinone-based inhibitors of protoporphyrinogen oxidase: Design, synthesis, and herbicidal activity

2020 ◽  
Vol 170 ◽  
pp. 104684 ◽  
Author(s):  
Li-xia Zhao ◽  
Jia-jun Hu ◽  
Zhi-xin Wang ◽  
Min-lei Yin ◽  
Yue-li Zou ◽  
...  
Keyword(s):  
Herbicidal Activity ◽  
Design Synthesis ◽  
Protoporphyrinogen Oxidase

Novel Schiff bases–based thiophenes: Design, synthesis and biological evaluation

2020 ◽  
Vol 67 (7) ◽  
pp. 1278-1288
Author(s):  
Divyaraj Puthran ◽  
Boja Poojary ◽  
Soukhyarani G. Nayak ◽  
Nikil Purushotham ◽  
Manjunath Bhat ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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