• Archives of Pharmacal Research
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• v.20 no.4
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• pp.330-337
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• 1997

Thiocarboxamidocinnamonitrile derivatives 2 under bar a-f reacted with 3-aminopyrazole derivative 3 under bar a-c to give the pyrazole[3, 2-b]pyrimidine derivatives 6 under bar a-p. Compounds 6 under bar a-p were used as starting material for syntheses of several heterocylic coompounds. Dehydrogenation of 6 under bar gave pyrazole[3, 2-b]pyrimidines 10 under bar a-d while its reaction with diethyl oxalate gave 11 under bar. Reactions of 6 under bar with formic acid gave pyrazolopyrimidines 17 under bar a-j, and pyrazolopyrimidopyrimidines 18 under bar a-j.

• The Korean Journal of Pesticide Science
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• v.8 no.4
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• pp.258-264
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• 2004

The pyrazole family was discovered as effective insecticides/acaricides, and fenpyroximate and tebufenpyrad were introduced in the market. In this study, new series of pyrazole oxime ethers were designed and synthesized. The pyrazolone 1 was prepared by the condensation of ethyl acetoacetate with methylhydrazine, and then subsequently subjected to the Vilsmeier-Haack chloroformylation yielding 4-formyl-5-chloro-pyrazole 2. The nucleophilic aromatic substitution of 2 generally allowed the introduction of a wide range of heterocycles into the pyrazole ring. The resulting pyrazole aldehydes 3a-i were readily converted to the corresponding pyrazole oxime derivatives 4a-i, and subsequently to 5-substituted pyrazole oxime ether derivatives 6a-i. The screening assay results clearly show that the activities of 6d were comparable to those of fenpyroximate (6a) against BPH, DBM, and TSSM. It indicates that 6d has a potential to be developed as an insecticidal agent.

• Archives of Pharmacal Research
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• v.10 no.1
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• pp.14-17
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• 1987

Several new imidazo [1, 2-b] pyrazole, pyrazolo [5, 1-c]-1, 2, 4-triazine and pyrazolo [5, 1-c] triazole derivatives were prepared from the reaction of 3-antipyrinyl-5-aminopyrazole or its diazonium salt with .alpha.-chloroacetyl derivatives.

• Journal of the Korean Chemical Society
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• v.62 no.2
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• pp.87-92
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• 2018

A series of pyrimidine annulated dihydropyrano[2, 3-c]pyrazole derivatives were synthesized and screened for their antimicrobial activity. The precursor, dihydropyrano[2, 3-c]pyrazole was synthesised under catalyst free condition using PEG-400 as reaction medium which facilitated improved yield compared to base catalyzed reaction. Wide scope of substrates, simple workup procedure and high yield even in the absence of catalyst are the major highlights of the protocol. Dihydropyrano[2, 3-c]pyrazoles on condensation with formic acid formed pyrimidine annulated dihydropyrano[2, 3-c]pyrazole derivatives. All the products are characterized using FTIR, $^1H-NMR$ and $^{13}C-NMR$ spectroscopic techniques. The molecules have shown good to moderate activity as antimicrobial agents when compared to the standard drug ciprofloxacin.

• Bulletin of the Korean Chemical Society
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• v.35 no.4
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• pp.1221-1224
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• 2014

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.75-77
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• 1993

The cycloaddition reaction of N-phenyl-C-cinnamonitrilimine 4 to coumarin leads to the for-mation of 3-styrylbenzopyrano[4,3-c]pyrazole derivative 6, whereas 3-phenylsulfonylcoumarin 9 or 3-bromocoumain 10 or 3-cyanocoumarin 11 gives 1-styrylbenzopyrano[3,4]pyrazole derivative 7. Also, the cycloaddition of 4 to 3-acetylocoumarin 15 and 3-benzoylocumain 16 gives the corresponding dihydropyrano[3,4-c]pyrazole adducts 17 and 18 respectively. Oxidation of 17 and 18 gives 7.

• Journal of Integrative Natural Science
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• v.7 no.3
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Journal of Integrative Natural Science
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• v.8 no.3
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• pp.204-208
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• 2015

Pyrazole, ${\beta}$-lactam, salicidine, pyren and oxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against COX-2 enzyme. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Archives of Pharmacal Research
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• v.12 no.3
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• pp.201-206
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• 1989

The reaction of acetoacetanilide (1) with the $\alpha$-cyanocinnamonitrile derivatives 2 yielded the Michael adducts 4 which could be converted into the pyrano [2, 3, -c] pyrazole derivatives 5 via their reaction with hydrazine hydrate. Cyclisation of 4 afforded the derivatives 10. The pyranopyrazoles 9 reacted with different activated nitrile derivatives (3a-c) to give the pyrano [2, 3-c] pyridine derivatives 13. 16 and 19 respectively. The biological activity of the synthesised heterocyclic derivatives was investigated and discussed.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.204-206
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• 1990

Certain pyrazolin-5-one and pyrazole derivatives bearing uracil-6-yl or tetrazol-5-yl moiety in position 1 have been synthesized. The anti-inflammatory activity of six representative compounds have been tested and the results are reported.