926257-97-8

Upstream product

• 89-25-8 edaravone 
• 371-41-5 4-Fluorophenol 
• 947-95-5 5-chloro-4-formyl-3-methyl-1-phenyl-1H-pyrazole 
• 6078-46-2 ethyl 3-(2-phenylhydrazono)butanoate 
• 100-63-0 phenylhydrazine 
• 942-32-5 5-methyl-2-phenyl-2H-pyrazol-3-ol 

Downstream Products

• 1246351-86-9 C₃₆H₃₂FN₄O₆PS 
• 1246351-84-7 C₂₈H₃₂FN₄O₆PS 
• 1240905-62-7 6-fluoro-3-methyl-1-phenylchromeno[2,3-c]pyrazol-4(1H)-one 
• 1621530-07-1 (E)-1-(4-fluorophenyl)-3-(3-methyl-1-phenyl-5-(3-(trifluoromethyl)phenoxy)-1H-pyrazol-4-yl)prop-2-en-1-one 
• 1621529-97-2 5-(4-fluorophenyl)-2-(4-methoxyphenyl)-3'-methyl-1'-phenyl-5'-(3-(trifluoromethyl) phenoxy)-3,4-dihydro-1′H,2H-3,4′-bipyrazole 
• 1621529-96-1 2-(4-bromophenyl)-5-(4-fluorophenyl)-3'-methyl-1'-phenyl-5'-(3-(trifluoromethyl) phenoxy)-3,4-dihydro-1'H,2H-3,4'-bipyrazole 
• 1621529-92-7 2,5-bis(4-fluorophenyl)-3'-methyl-1'-phenyl-5′-(3-(trifluoromethyl)phenoxy)-3,4-dihydro-1'H,2H-3,4'-bipyrazole 
• 1426300-78-8 C₂₆H₂₄FN₃O₄S₂ 
• 1426300-54-0 C₂₅H₂₂FN₃O₄S₂ 
• 1426300-38-0 C₂₂H₁₆FN₃O₄S₂ 

Relevant academic research and scientific papers

Design, synthesis and evaluation of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties as antibacterial agents

Abstract: In the present investigation, a series of dihydrotriazine derivatives-bearing 5-aryloxypyrazole moieties were synthesized and their structures were confirmed by different spectral tools. The biological evaluation in vitro revealed that some of the target compounds exerted good antibacterial and antifungal activity in comparison with the reference drugs. Among these novel hybrids, compound 10d showed the most potent activity with minimum inhibitory concentration values (MIC) of 0.5?μg/mL against S. aureus 4220, MRSA 3506 and E. coli 1924 strain. The cytotoxic activity of the compounds 6d, 6m, 10d and 10g was assessed in MCF-7 and HeLa cells. Growth kinetics study showed significant inhibition of bacterial growth when treated with different conc. of 10d. In vitro enzyme study implied that compound 10d exerted its antibacterial activity through DHFR inhibition. Moreover, significant inhibition of biofilm formation was observed in bacterial cells treated with MIC conc. of 10d as visualized by SEM micrographs. Graphic abstract: Twenty-nine target compounds were designed, synthesized and evaluated in terms of their antibacterial and antifungal activities.[Figure not available: see fulltext.].

Synthesis of 1H-pyrazolo[1,2-b]phthalazine-5,10-dione derivatives: Assessment of their antimicrobial, antituberculosis and antioxidant activity

A new series of pyrazolo[1,2-b]phthalazine derivatives (4a-p) bearing the 5-aryloxypyrazole nucleus was synthesized by one-pot, three-component, base-catalyzed cyclo condensation reaction of 3-methyl-5-aryloxy-1-aryl-1H-pyrazole-4-carbaldehyde (1a-d), mal

Green method for the synthesis of chromeno[2,3- C ]pyrazol-4(1 H)-ones through ionic liquid promoted directed annulation of 5-(aryloxy)-1 H -pyrazole-4-carbaldehydes in aqueous media

The first classical heterocyclic ionic liquid (IL) promoted C-H bond oxidant cross-coupling reaction for the intramolecular annulation of 5-(aryloxy)-1H-pyrazole-4-carbaldehydes to chromeno[2,3-c]pyrazol-4(1H)-ones has been disclosed. The promoter 1,3-dibutyl-1H-benzo[d][1,2,3]triazol-3-ium bromide can be easily recycled and reused with the same efficacies for at least five cycles in aqueous medium. The strategy works smoothly and provides an applicable protocol to construct a wide range of products.

Green synthesis and pharmacological screening of polyhydroquinoline derivatives bearing a fluorinated 5-aryloxypyrazole nucleus

A novel series of polyhydroquinoline scaffolds 8a-p has been designed and synthesized under ultrasonic irradiation by a one-pot three-component cyclocondensation reaction of 3-methyl-5-substituted aryloxy-1-phenyl-1H-pyrazole-4-carbaldehydes 3a-d with malononitrile 7 and various enhydrazinoketones 6a-e in the presence of piperidine as basic catalyst. All the synthesized compounds have been characterized by various spectroscopic techniques and elemental analysis. All the synthesized compounds were evaluated for their in vitro antibacterial activity against a panel of pathogenic strains of bacteria and fungi, in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain and also for their in vitro antimalarial activity against Plasmodium falciparum. Compounds 8c, 8i, 8j, 8l and 8m exhibited excellent antimalarial potency. The cytotoxicity of the synthesized compounds was tested using a bioassay of S. pombe cells at the cellular level. Compounds 8i, 8j, 8k and 8l were found to have maximum toxicity, while compounds 8e, 8m, 8c were found to be less cytotoxic. Some of them displayed luminous antibacterial activity and reasonable antituberculosis activity as compared with the first line drugs.

Design, synthesis, and antibacterial evaluation of new Schiff's base derivatives bearing nitroimidazole and pyrazole nuclei as potent E. coli FabH inhibitors

New Schiff's base derivatives 5a-j have been synthesized by reaction between 5-aryloxypyrazole-4-carbaldehydes 3a-j and 2-(2-methyl-5-nitro-1Himidazol- 1-yl)acetohydrazide 4 in the presence of nickel (II) nitrate as a catalyst in ethanol at room temperatu

Design, synthesis and bioactivities of novel dichloro-allyloxy-phenol-containing pyrazole oxime derivatives

In this study, in order to find novel biologically active pyrazole oxime compounds, a number of dichloro-allyloxy-phenol-containing pyrazole oximes were designed and synthesized according to the method of active group combination. All of the target compounds were confirmed by 1H-NMR, 13C-NMR and elemental analysis. In addition, bioassays showed that all of the newly synthesized compounds had no acaricidal activity against Tetranychus cinnabarinus and low insecticidal activity against Aphis craccivora at tested concentrations. However, most of them displayed excellent insecticidal activity against Oriental armyworm at a concentration of 500 μg/mL, and some designed compounds still exhibited potent insecticidal activity against Oriental armyworm even at the dose of 20 μg/mL, especially compounds 7f, 7n and 7p had 100%, 90% and 90% inhibition rates, respectively, which were comparable to that of the control pyridalyl.

Synthesis and evaluation on anticonvulsant activities of pyrazolyl semicarbazones

In this paper, a series of 2-[(5-phenoxy-3-methyl-1-phenyl-1H-pyrazol-4-yl)-methylene]hydrazine carboxamides were synthesized and evaluated for their anticonvulsant activities using the maximal electroshock method. Their neurotoxicities were determined ap

Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening

A novel series of fluoro substituted pyrazolylpyrazolines 7a-l was synthesized in good to excellent yield (77-88%) from pyrazole chalcones 5a-d and substituted phenyl hydrazine hydrochlorides 6a-c under microwave irradiation. The newly synthesized compounds were screened for their preliminary in vitro antibacterial activity against a panel of pathogenic stains of bacteria and fungi, antituberculosis activity against Mycobacterium tuberculosis H37Rv and antimalarial activity against Plasmodium falciparum. Compounds 7a, 7b, 7g, 7h, 7j and 7k displayed excellent activity against P. falciparum stain as compared to quinine IC50 0.268. Good antitubercular activity was exhibited by compounds 7a, 7e, 7h and 7k. Some of them also exhibited superior antibacterial activity as compared to the first line drugs.

Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA)

With an intention to synergize the anti-bacterial activity of 5-aryloxy pyrazole and rhodanine derivatives, eight series of hybrid compounds have been synthesized and evaluated for their antibacterial activity. The majority of the synthesized compounds showed good inhibitory activity against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA, QRSA) with minimum inhibitory concentration (MIC) values in the range of 1-32 μg/mL. The cytotoxicity test suggests that these compounds exhibited in vitro antibacterial activity at non-cytotoxic concentrations. These studies therefore suggest that rhodanine-based 5-aryloxy pyrazoles are interesting scaffolds for the development of novel Gram-positive antibacterial agents.

Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents

Three novel series of 5-aryloxypyrazole derivatives have been synthesized and tested for their antibacterial activity. The majority of the synthesized compounds showed potent inhibitory activity against Gram-positive bacteria Staphylococcus aureus 4220, especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compounds IIIb, IIIg and IIIm showed the most potent levels of activity (MIC = 1 μg/mL) against the multidrug-resistant strains. And cytotoxic activity assay showed that the compounds tested did not affect cell viability on the Human cervical (HeLa) cells at their MICs. The current study therefore suggests that 5-aryloxypyrazoles bearing a rhodanine-3-aromatic acid moiety are promising scaffolds for the development of novel Gram-positive antibacterial agents.