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

• Archives of Pharmacal Research
• /
• 제17권4호
• /
• pp.278-280
• /
• 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
• /
• 제34권10호
• /
• pp.2915-2920
• /
• 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.

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

• Bulletin of the Korean Chemical Society
• /
• 제23권6호
• /
• pp.911-914
• /
• 2002

• 농약과학회지
• /
• 제3권1호
• /
• pp.96-101
• /
• 1999

새로운 합성방법을 개발하여 pyrazolate 제초제의 곁가지를 변화시킨 새로운 구조의 3-trifluoro-methylpyrazole 유도체들과 4-benzenecarbinolpyrazole 유도체 등을 합성하여 전작과 답작상태에서 제초활성 시험을 하였다. 밭조건에서는 발아전처리의 경우 4 kg/ha의 약량에서도 제초효과를 나타내지 않았으며 발아후처리에서는 제초효과가 있었으나 미약하였다. 답작상태에서는 4 kg/ha의 약량에서 제초효과가 있었으며 특히 4-benzoylpyrazole의 benzene의 4위치에 electron-donating group인 methoxy가 치환된 화합물의 경우 활성과 선택성이 매우 좋았다. 그러나, methoxy가 두 개 이상 치환되거나 다른 electron-donating group인 sulfide기가 치환된 화합물들의 제초활성은 약하였다.

• Bulletin of the Korean Chemical Society
• /
• 제26권12호
• /
• pp.2078-2080
• /
• 2005

• Archives of Pharmacal Research
• /
• 제16권3호
• /
• pp.251-253
• /
• 1993

Several new coumarinoyl and coumarionyl-1, 2, 4-triazole derivatives were synthesised via dipolar cycloaddition reactions with 3-coumainohydraziodoyl halide. Structure were based on elemental analysis and spectral data.

• Bulletin of the Korean Chemical Society
• /
• 제33권4호
• /
• pp.1345-1348
• /
• 2012

• Bulletin of the Korean Chemical Society
• /
• 제33권6호
• /
• pp.2067-2070
• /
• 2012