Synthesis, Characterization and Antimicrobial activities of some new Pyrazole-1-carbothioamide derivatives.

2021 ◽  
Vol 9 (11) ◽  
pp. 1720-1723
Author(s):  
Vikram R. Dangar
Keyword(s):  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Mass Data

Abstract: Some new 5-Aryl-3-[4’-(o-chlorobenzyloxy)-3’-methoxy-phenyl]-1-carbothioamide-4, 5-dihydro-1H-pyrazole derivatives were prepared. All the prepared compounds were characterized by their spectral (I.R., N. M. R., Mass) data and screened for their antimicrobial activities. Keywords: Chalcones & Pyrazoline derivatives, Antimicrobial activities.

scholarly journals Novel Acetohydrazide Pyrazole Derivatives: Design, Synthesis, Characterization and Antimicrobial Activity

2019 ◽  
Vol 31 (12) ◽  
pp. 2740-2744
Author(s):  
Anil Verma ◽  
Vinod Kumar ◽  
Ramesh Kataria ◽  
Joginder Singh
Keyword(s):  
Mass Spectrometry ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Reaction Conditions ◽  
Design Synthesis ◽  
Structure Activity ◽  
Electron Withdrawing Group ◽  
Sar Study

Eleven acetohydrazide linked pyrazole derivatives were designed and synthesized via condensation of acetohyadrazide with different substituted formyl pyrazole derivatives under mild reaction conditions. Synthesized compounds were characterized on the basis of IR, NMR (1H & 13C) and mass spectrometry. The antimicrobial activities of all the compounds were screened against four bacterial and two fungal strains. Among the synthesized compounds, three compounds viz. 6b, 6c and 6d were found as efficient antimicrobial agents in reference to the standard drugs viz. ciprofloxacin and amphotericin-B. Further, structure-activity relationship (SAR) study revealed that electron-withdrawing group enhances the antimicrobial potential of synthesized derivatives as compared to other groups present in the ring. Hence, among compounds 6b-c, compound 6d could be explored further against other microbes to prove its vitality.

scholarly journals A RECENT UPDATE: ANTIMICROBIAL AGENTS CONTAINING PYRAZOLE NUCLEUS

2018 ◽  
Vol 11 (12) ◽  
pp. 88 ◽  
Author(s):  
Bayu Ardiansah
Keyword(s):  
Broad Spectrum ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Bioactive Molecules ◽  
Pyrazole Derivatives ◽  
Research Results ◽  
Antimicrobial Performance

Objective: In this review, we report antimicrobial candidates containing pyrazole nucleus integrated with various functionalities.Methods: research results by numerous scientists have been summarized from international journals indexed in reputed database such as Scopus and Web of Science.Results: Pyrazole derivatives are much of interest as potent bioactive molecules. They have shown large bioactivities especially antimicrobial performance against broad spectrum of bacterial strains.Conclusion: Several designed pyrazole derivates possessed good to superior antimicrobial activities.

Synthesis, Characterization and Biological Evaluation of Ethyl-4'-(cyclopropane carboxamido-N-yl)-5-ary-3-oxo-3,4,5,6-tetrahydro-biphenyl-4-carboxylate

2019 ◽  
Vol 4 (4) ◽  
pp. 240-243
Author(s):  
P.M. Akbari ◽  
V.R. Shah
Keyword(s):  
Sodium Hydroxide ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Antimicrobial Drugs ◽  
Gram Negative ◽  
Mass Data ◽  
Condensation Method ◽  
Cyclohexenone Derivatives

A series of new substituted cyclohexenone derivatives have been synthesized by the reaction of various substituted chalcones with ethylacetoacetate. Some new N-(4-(3-aryl-acryloyl)phenyl)cyclopropane carboxamide were prepared by Claisen-Schmidt condensation method in presence of sodium hydroxide in ethanol solvent under stirring. The synthesized compounds were characterized by their spectral (IR, NMR, Mass) data and screened for their antimicrobial activities against Gram-positive and Gram-negative bacteria by using standard antimicrobial drugs.

scholarly journals A Facial Synthesis and Antimicrobial Activity of Some Pyrazole Derivatives Carrying Indole

2010 ◽  
Vol 7 (3) ◽  
pp. 745-750 ◽  
Author(s):  
K. Narasimha Sarma ◽  
M. C. S. Subha ◽  
K. Chowdoji Rao
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Carboxylic Acid ◽  
Hydrazine Hydrate ◽  
Elemental Analysis ◽  
Antimicrobial Activities ◽  
Subsequent Treatment ◽  
Spectral Studies ◽  
Pyrazole Derivatives

The title compounds (7a-h) were prepared by esterification of indole-5-carboxylic acid (1) and subsequent treatment with hydrazine hydrate in methanolviathe hydrazide (3). Finally hydrazide (3) condensed with different substituted aldol (6) in acetic acid / PTSA catalytic media produced (3,5-subsituted-4,5-dihydropyrazol-1-yl)(1H-indol-5-yl)methanone (7a-h) in good yields. All the newly synthesized compounds are by elemental analysis and spectral studies and evaluated for antimicrobial activities.

Synthesis and Biological Evaluation of Some Pyrazole Derivatives, Containing (Thio) Semicarbazide, as Dual Anti-Inflammatory Antimicrobial Agents

2019 ◽  
Vol 16 (9) ◽  
pp. 1020-1030
Author(s):  
Zhaochang Liang ◽  
Yuping Huang ◽  
Shiben Wang ◽  
Xianqing Deng
Keyword(s):  
Antiinflammatory Activity ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pyrazole Derivatives ◽  
Reference Drug ◽  
Tnf Α ◽  
Anti Inflammatory

Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1H NMR, 13C NMR and HRMS. In vitro LPS-induced TNF-α model and in vivo xylene-induced ear-edema model were used to evaluate their antiinflammatory activity. Their in vitro antimicrobial activities were evaluated using a serial dilution method against several gram-positive strains, gram-negative strains and a fungi strain. Results: Bioassays indicated that most of the compounds markedly inhibited the expression of TNF- α at the concentration of 20 µg/mL Compounds 5i, 6b, and 7b had comparable in vivo antiinflammatory activity to the reference drug dexamethasone at the dose of 50 mg/kg. In addition, several compounds showed antimicrobial activity against different strains, and compounds 5g and 5h exhibited potent inhibitory activities with the MIC value of 8 µg/mL against the Streptococcus pneumoniae CMCC 31968 and Staphylococcus aureus CMCC 25923, respectively. Compound 7b, which exhibited both anti-inflammatory and antimicrobial activities, should be studied as it is or after derivatization. Conclusion: It can be concluded that pyrazoles, with (thio)-semicarbazone moieties, have the potential to be developed into new anti-inflammatory agents.

Nano-SnCl4/SiO2 as a Catalyst for One-Pot Synthesis of Substituted 1H-Pyrazoles as Antifungal and Cytotoxic Agents

2020 ◽  
Vol 17 (6) ◽  
pp. 459-465
Author(s):  
Soghra Khabnadideh ◽  
Zeinab Faghih ◽  
Leila Zamani ◽  
Kamiar Zomorodian ◽  
Bi Bi Fatemeh Mirjalili ◽  
...  
Keyword(s):  
Cell Lines ◽  
Human Cancer ◽  
Antimicrobial Activities ◽  
Cytotoxic Agents ◽  
Cytotoxic Activities ◽  
Pyrazole Derivatives ◽  
One Pot ◽  
Human Cancer Cell Lines ◽  
Cancerous Cell ◽  
Anti Cancer

A simple and efficient method was developed for the synthesis of pyrazole derivatives via a one-pot reaction of 1,3-diketone and substituted hydrazines in the presence of nano-SnCl4/SiO2 as a mild catalyst. A series of some pyrazole derivatives (P1-P11) was synthesized and evaluated as antifungal and anti-cancer agents. Compounds P10 and P11 were demonstrated. The antimicrobial activities of the synthetic compounds showed that compounds P10 and P11 most excellently inhibited the growth of dermatophytes or Aspergillus species, respectively. Therefore, the cytotoxic activities of these compounds on two human cancer cell lines, A549 (lung cancer) and MCF-7 (breast cancer) were further assessed. Hence, results demonstrated that beside antifungal activity, P10 had also desirable cytotoxic effect on investigated cancerous cell lines, even higher than cisplatin.

ChemInform Abstract: Synthesis and in vitro Antimicrobial Activities of New (Cyano-NNO-azoxy) Pyrazole Derivatives.

ChemInform ◽  
2011 ◽  
Vol 42 (44) ◽  
pp. no-no
Author(s):  
Donatella Boschi ◽  
Stefano Guglielmo ◽  
Stefania Aiello ◽  
Giulia Morace ◽  
Elisa Borghi ◽  
...  
Keyword(s):  
Antimicrobial Activities ◽  
Pyrazole Derivatives

Synthesis of Novel Tetra-Substituted Pyrazole Derivatives from 2,3- Furandione

2019 ◽  
Vol 16 (11) ◽  
pp. 891-897 ◽  
Author(s):  
Hasan Genç ◽  
Volkan Taşdemir ◽  
İsrafil Tozlu ◽  
Erdal Ögün
Keyword(s):  
Escherichia Coli ◽  
Saccharomyces Cerevisiae ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Solid State ◽  
Carboxylic Acid ◽  
Micrococcus Luteus ◽  
Antimicrobial Activities ◽  
Pyrazole Derivatives ◽  
Gram Positive Bacteria

Synthesis of pyrazole-3-carboxylic acid was progressed via two different protocols, one of which is solid state. Pyrazole-3-carboxylic acid was converted into different derivatives such as ester, urea, amide and nitrile. The amide compound was converted to nitrile using SOCl2 and DMF. Solid state heating of carboxylic acid gave decarboxylated product. Cyclization of tetra-substituted pyrazole with hydrazines resulted in pyrazolopyridazinones. The antimicrobial activities of the synthesized pyrazole derivatives against Bacillus cereus, Escherichia coli, Micrococcus luteus, Staphylococcus aureus, and Saccharomyces cerevisiae were evaluated. One of the pyrazole derivatives which possess nitro group showed antimicrobial activity in only B. cereus, a Gram-positive bacteria, with an MIC of 128 μg/mL.

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