Design, synthesis and bioassay of novel 1‐(3‐chloropyridin‐2‐yl)‐5‐amino‐4‐pyrazole derivatives containing a 1,3,4‐thiadiazole thioether or sulfone moiety

2021 ◽  
Author(s):  
Huanlin Zheng ◽  
Jiqing Kuang ◽  
Hong Zhang ◽  
Xue Niu ◽  
Zhibing Wu
Keyword(s):  
Pyrazole Derivatives ◽  
Design Synthesis

scholarly journals Design, Synthesis and Anticandidal Evaluation of Indazole and Pyrazole Derivatives

2021 ◽  
Vol 14 (3) ◽  
pp. 176
Author(s):  
Karen Rodríguez-Villar ◽  
Alicia Hernández-Campos ◽  
Lilián Yépez-Mulia ◽  
Teresita del Rosario Sainz-Espuñes ◽  
Olivia Soria-Arteche ◽  
...  
Keyword(s):  
Bloodstream Infections ◽  
Antifungal Drugs ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Bioisosteric Replacement ◽  
Current Therapies ◽  
Anticandidal Activity ◽  
Resistant Strains ◽  
A Priority

Candidiasis, caused by yeasts of the genus Candida, is the second cause of superficial and mucosal infections and the fourth cause of bloodstream infections. Although some antifungal drugs to treat candidiasis are available, resistant strains to current therapies are emerging. Therefore, the search for new candicidal compounds is certainly a priority. In this regard, a series of indazole and pyrazole derivatives were designed in this work, employing bioisosteric replacement, homologation, and molecular simplification as new anticandidal agents. Compounds were synthesized and evaluated against C. albicans, C. glabrata, and C. tropicalis strains. The series of 3-phenyl-1H-indazole moiety (10a–i) demonstrated to have the best broad anticandidal activity. Particularly, compound 10g, with N,N-diethylcarboxamide substituent, was the most active against C. albicans and both miconazole susceptible and resistant C. glabrata species. Therefore, the 3-phenyl-1H-indazole scaffold represents an opportunity for the development of new anticandidal agents with a new chemotype.

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.

Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAFV600E inhibitors

2014 ◽  
Vol 22 (21) ◽  
pp. 6201-6208 ◽  
Author(s):  
Shu-Fu Wang ◽  
Yin-Ling Zhu ◽  
Ping-Ting Zhu ◽  
Jigar A. Makawana ◽  
Ya-Liang Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Design, synthesis, characterization, in vitro screening, molecular docking, 3D-QSAR, and ADME-Tox investigations of novel pyrazole derivatives as antimicrobial agents

2022 ◽  
Author(s):  
Mohammed CHALKHA ◽  
Mohamed Akhazzane ◽  
Fatima Zahrae Moussaid ◽  
Ossama Daoui ◽  
Asmae Nakkabi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antimicrobial Agents ◽  
3D Qsar ◽  
Spectroscopic Techniques ◽  
In Vitro Screening ◽  
Pyrazole Derivatives ◽  
Design Synthesis ◽  
Practical Procedure

In this work, we report the synthesis of some new pyrazole derivatives via an efficient and practical procedure. The structures of the obtained compounds were established using different spectroscopic techniques...

New quinoline-2-one/pyrazole derivatives; design, synthesis, molecular docking, anti-apoptotic evaluation, and caspase-3 inhibition assay

2020 ◽  
Vol 94 ◽  
pp. 103348 ◽  
Author(s):  
Ashraf A. Aly ◽  
Samia M. Sayed ◽  
El-Shimaa M.N. Abdelhafez ◽  
Sara Mohamed Naguib Abdelhafez ◽  
Walaa Yehia Abdelzaher ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Caspase 3 ◽  
Pyrazole Derivatives ◽  
Inhibition Assay ◽  
Design Synthesis
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