• 대한화학회지
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• 제57권5호
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• pp.599-605
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• 2013

Some N-acetyl pyrazoles including 1-(3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-$^1H$-pyrazole- 1-yl) ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones like substituted styryl 3,4- dichlorophenyl ketones using hydrazine hydrate and acetic anhydride in presence of catalytic amount of fly-ash: $H_2SO_4$ catalyst. The yield of these N-acetyl pyrazole derivatives are more than 75%. The synthesised N-acetyl pyrazoline derivatives were characterized by their physical constants and spectral data.

• Archives of Pharmacal Research
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• 제17권5호
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• pp.298-303
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• 1994

4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

• 대한화학회지
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• 제55권2호
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• pp.256-261
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• 2011

Bis acetylated hybrid pyrazoles 을 합성하여 이들 화합물에 대해 녹는점, 원소분석, MS, FT-IR, one-dimensional $^1H,-$ 및 $^{13}C$-NMR로 분석하였다. 합성한 화합물들에 대해 in vitro 항균활성을 Candida sp. namely Candida albicans, Candida glabrata, Candida parapsilosis, Candida dubliniensis 및 Candida tropicali 균에 대해 수행하였다. Pyrazoles의 페닐고리에 작용기($-CH_3$, $-OCH_3$, -F, -Cl, 및 Br)가 있는 화합물은 Candida species에 대해서 강한 활성을 나타내었다.

• Bulletin of the Korean Chemical Society
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• 제32권12호
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• pp.4366-4370
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• 2011

A simple, green and cost-effective protocol was used for the aromatization of 1,3,5-trisubstituted-2-pyrazolines to the corresponding pyrazoles by in situ generation of iodine ($I^+$) from $H_2O_2$/AcOH or SSA or oxalic acid /KI or NaI system under thermal condition with moderate to good yields.

• Archives of Pharmacal Research
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• 제24권3호
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• pp.180-189
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• 2001

A new series of pyridazine, pyrazoles, pyrazolidine-3,5-dione, Semicarbazide, thiosemicarbazides, hydantoin, thiohydantoins, 1,2,4-triazoles, S-triazolo[3,4-b]-1,3,4-thiadiazoles incorporated indirectly into salicylamide moiety at position 2 were synthesized. Also the synthesis of novel series of 3-salicylamido-2-hydroxypropyl-amino derivatives were prepared. Several of these compounds were screened for antiinflammatory, analgesic, antipyretic and ulcerogenic activities.

• 대한화학회지
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• 제54권6호
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• pp.737-743
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• 2010

5-Amino-1,3-diaryl-pyrazoles 1a-c 와 다양한 aryl amine의diazonium salts를 반응시켜서 1,3-diaryl-5-amino-4-arylazopyrazoles 3a-l을 합성하였으며, 몇 가지 화합물은 5-amino-1,3-diaryl-4-nitroso-1H-pyrazoles 2a-c와 aryl amine의 diazonium salts를 반응시켜서 얻었다. 합성한 azo 유도체 화합물 3a-l을 DMF 용매 속에서 cupric acetate와 산화반응시켜서 2,4,6-triaryl-2,4-dihydropyrazolo [4,3-d]-1,2,3-triazoles 4a-l을 합성하였으며, 합성한 cyclic triazoles에 대한 형광 특성을 측정하였다. 한편, Diazotization of sodium nitrite/ortho-phosphoric acid 조건에서 5-amino-1,3-diaryl-1H-pyrazoles 1a-c를 diazotization화 반응시킨 다음에, aryl amines과 반응시켜서 o-aminoazo compounds 5a-f를 합성하였다. 합성한 화합물 5a-f를 pyridine/cupric acetate 반응 조건에서 반응시켜서 triazole 6a-f들을 합성하였으며, 얻어진 화합물 6a-f을 aryl diazonium salts과 반응시켜서 화합물 7a-j을 합성하였다. 합성한 염료 화합물을 polyesters에 분산염료와 정착성을 측정하였다.

• Bulletin of the Korean Chemical Society
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• 제33권11호
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• pp.3629-3634
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• 2012

A series of new 4-(pyridin-4-yl)-(3-methoxy-5-methylphenyl)-1H-pyrazoles (6a-k & 7a-l) has been rationally designed based on the structure of the lead compound KIST301080, a selective ROS receptor tyrosine kinase inhibitor, in order to study the activity of ROS of this new class of inhibitors. The compounds were synthesized and screened against ROS kinase, where compound 6h showed moderate inhibitory activity with an $IC_{50}$ value of $6.25{\mu}M$. The study emphasized the importance of the acetonitrile group at the pyrazole ring and also the importance of having a hydrogen bond donor on the distal phenyl ring linked to the pyridine moiety.

• Bulletin of the Korean Chemical Society
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• 제34권2호
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• pp.437-442
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• 2013

A new series of 4-(2-(substituted)pyridin-4-yl)-3-(3-methoxy-5-methylphenyl)-1H-pyrazoles (4a-f) and their 1,2-isoxazole analogues (5a-f) has been rationally designed, synthesized and screened against both ROS and MAPK14 kinases. Compounds 4b, 4c and 4e showed moderate inhibitions against both ROS and MAPK14 kinases. Compound 4e has showed the strongest inhibitions with IC50 values of 1.25 ${\mu}M$ and 3.00 ${\mu}M$ against ROS and MAPK14 kinases, respectively. A brief structure-activity relationship study and a molecular modeling study were made revealing a group of essential structural features for good kinase inhibitory activity within this new class of kinase inhibitors.

• Archives of Pharmacal Research
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• 제17권4호
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• pp.278-280
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• 1994

1,5-diketones(3) undewent cyclization to 4H-pyrano[3,2-d]pyrazoles (4a-d),4H-piperidino[3, 2-d]pyrazole (5) and pyrazolo[5,4-d]thiopyran (6) upon treatment with P/sub 2/O/sub 5/, CH/sub 3/COONH/sub 4/ and /or P/sub 2/S/sub 5/. Moreover, treatment of (4) with CH/sub 3/COONH/sub 4/ and/or P/sub 2/S/sub 5/ afforded (5) and (6). The structures of the hitherto unknown ring systems have been confirmed by analytical and spectral data.

• Bulletin of the Korean Chemical Society
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• 제34권10호
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• pp.2915-2920
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• 2013

Convenient synthetic method for 4-arylethylpyrazoles and 4-styrylpyrazoles was developed using ${\alpha}$-alkenyl-${\alpha},{\beta}$-enones readily accessed from the Morita-Baylis-Hillman reaction. For the synthesis of 4-arylethylpyrazole, the reactions with arylhydrazines needed to be carried out in o-dichlorobenzene under $N_2$ balloon atmosphere. On the other hand, 4-styrylpyrazoles required the reactions in ethanol under $O_2$ balloon atmosphere.