The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives

Yu, Ligang; Ni, Tengfeng; Gao, Wei; He, Yonghong; Wang, Yingying; Cui, Hai-Wei; Yang, Cai‐Guang; Qiu, Wen‐Wei

doi:10.1016/j.ejmech.2014.11.015

Cited by 43 publications

(19 citation statements)

References 19 publications

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“…A series of novel diterpene derivatives containing pyrazole ring were synthesized and investigated for their activity against S. aureus Newman strain and multidrug-resistant strains ( NRS-1 , NRS-70 , NRS-100 , NRS-108 and NRS-271 ). Among the compounds tested, compound 195 showed the most potent activity with MIC values of 0.71–3.12 µg/mL against five multidrug-resistant S. aureus [ 99 ]. Elshaier et al described the synthesis and antimicrobial activity of new series of pyrazole-thiobarbituric acid derivatives.…”

Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

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Section: Pharmacological Activitiesmentioning

confidence: 99%

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

et al. 2018

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“…In recent years, literature revealed that pyrazole derivatives had a wide range of biological activities, such as antibacterial [ 5 , 6 , 7 ], fungicidal [ 8 , 9 , 10 ], insecticidal [ 10 , 11 , 12 , 13 ], antiviral [ 14 , 15 ], and herbicidal [ 16 , 17 ] activities. In our previous work, we reported a series of pyrazole derivatives which had better insecticidal activity against Plutella xylostella [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity

Yang

Gan

2018

Molecules

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In this study, a series of novel pyrazole-hydrazone derivatives containing an isoxazole moiety were synthesized. Antiviral bioassays indicated that some of the title compounds exhibited better in vivo antiviral activities against tobacco mosaic virus (TMV). In particular, compounds 6a, 6c and 6q exhibited the best curative activity, protection activity, and inactivation activity against TMV, respectively, which were superior to those of Ningnanmycin. This study demonstrated that this series of novel pyrazole-hydrazone derivatives containing an isoxazole amide moiety could effectively control TMV.

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“…Several recent studies demonstrated drug resistance for their recommended antibiotic therapy with increasing prevalence in parasitic protozoa including Trypanosoma, Plasmodium, Toxoplasma gondii, Leishmania, and Entamoeba. [13][14][15][16] During the early stages of medicinal chemistry development, scientists were primarily concerned with the isolation of medicinal agents found in plants. Today, scientists in this field are also equally concerned with the creation of new synthetic drug compounds.…”

Section: Original Articlementioning

confidence: 99%

Untitled

Jain¹

2020

IJGP

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Objective: The objective of the paper was to design, synthesis, and characterization of new 1,3,5-trisubstituted-2pyrazolines derivative and evaluate for antibacterial activity. Materials and Methods: The 1,3,5-tri-substituted-2pyrazolines derivatives have been synthesized by the reaction of chalcone derivatives with succinic hydrazide in the environment of pyridine. A total of 20 compounds have been synthesized and characterized by the infrared, 1H-nuclear magnetic resonance, and mass spectral analysis. Antibacterial activity of the compounds carried out on five Grampositive bacterial strains, that is, Staphylococcus aureus, Staphylococcus faecalis, Bacillus subtilis, Proteus vulgaris, and Bacillus pumilus and two Gram-negative bacterial strains, that is, Escherichia coli and Klebsiella pneumoniae in two different concentrations, that is, 50 and 100 µg/ml by agar diffusion method using cup-plate method. Norfloxacin and ciprofloxacin were used as standard antibacterial drug. Results and Discussion: The data of antibacterial activity against the Gram-positive bacterial strains (S. aureus, S. faecalis, B. subtilis, P. vulgaris, and B. pumilus) suggested the order of activity of compounds: BR-3 >BR-2>BR-1>CL-4>BR-4>CL-3> CL-2>CL-5>CL-6>ME-3>ME-2>ME-4>ME-5>ME-6>ME-7>CL-7>CL-8>CL-1>ME-8>ME-1. The compounds series BR-1 to BR-4 has shown the highest activity.

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The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives

Cited by 43 publications

References 19 publications

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Novel Pyrazole-Hydrazone Derivatives Containing an Isoxazole Moiety: Design, Synthesis, and Antiviral Activity

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