• Title/Summary/Keyword: Pyrazole

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Fetal growth retardation induced by flupyrazofos, a new organophosphorus insecticide, in rats.

  • Chung, Moon-Koo;Kim, Jong-Choon;Han, Sang-Seop
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.05a
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    • pp.122-122
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    • 2001
  • Flupyrazofos is a new type of pyrazole organophosporus insecticide, which has a high activity against the diamond-back moth (Plutella xylostella). The potential of this agent to induce developmental toxicity was investigated in the Sprague-Dawley rat.(omitted)

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Aromatization of 1,3,5-Trisubstituted of 4,5-Dihydro-1H-Pyrazoles by In-Situ Generation of I+ from Hydrogen Peroxide/Acids/Iodide Potassium or Sodium Systems

  • Maleki, Behrooz;Veisi, Hojat
    • Bulletin of the Korean Chemical Society
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    • v.32 no.12
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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.

Synthesis of C-(2-Furyl)-N-(4-nitrophenyl)methanohydrazonyl Bromide. Reactions with Nucleophiles and Active Methylene Compounds

  • Hassaneen, Hamdi M.;Shawali, Ahmad S.;Elwan, Nehal M.;Ibrahim, Al Hossien A.
    • Archives of Pharmacal Research
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    • v.14 no.3
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    • pp.266-270
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    • 1991
  • Synthesis of C-(2-furyl)-N-(4-nitrophenyl)methanohydrazonyl bromide 2 is described. Treatment of 2 with uncleophiles affords the corresponding substitution products 3-7. Also, compound 2 reacts with selenocyanate anion and thiocyanate anion and give the corresponding selenadiazoline and thiadiazoline 8 and 9, respectively. Moreover, reaction of 2 with enolates of various active methylene compounds afforded the pyrazole derivatives 17-20.

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Reactions with Hydrazidoyl Halides (V): Synthesis of Some Amidrazones, Hydrazides, Pyrazoles and Pyrazolo [3, 4-d] pyridazine Derivatives

  • Attaby, Fawzy A.;Zaki, Mayssoune Y.;Abdelhamid, Abdou O.;Ramadan, Nazmy A.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.314-318
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    • 1990
  • 2-Bromo (2'-benzofury)gloxal-2-aryhydrazones I reacted with nucleophiles displacing the bromide. Treatment of I with active methylene compounds yield the pyrazole derivatives VIII-XI. Compounds XII-XIV reacted with hydrazine to give pyrazolo (3, 4-dipyridazine derivative XIV-XIV. The structures of the products were assigned and confirmed on the basis of their elemental analysis and spectral data.

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Reactions with Cyanothioacetamide Derivatives: Synthesis of Several New Pyridine and Annelated Pyridine Derivatives

  • Attaby, Fawzy A.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.342-346
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    • 1990
  • Several new pyridine, pyridinethione, pyrazole [3, 4-b]-pyridine, pyrido [1, 2-a]-1, 3-thiazine and pyrido[1, 2-a] pyridine thione derivatives have be synthesised via the reactions of 2-methyl-3-ethoxycarbonyl-4-phenyl-5-cyano-1, 4, 5, 6-tetrahydro-pyridine-6-one 2 with different rfeagents. The structures of the newly synthesised derivatives were established on the basis of elemental analyses and spectral data studies.

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Synthesis and Biological Activities of New Substituted Indoles

  • Hishmat, Orchidee H.;Nakkady, Sally S.;El Shabrawy, Osama A.;Mahmoud, Sawsan S.
    • Archives of Pharmacal Research
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    • v.15 no.1
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    • pp.104-108
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    • 1992
  • 2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

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Effect of Panax Ginseng in Mouse Liver with Ethnol-Induced Monoamine Oxidase Activity (Ethanol이 유도한 간장중 MAO 활성변동에 미치는 인삼의 영향)

  • Huh, Keun;Lee, Sang-Il;Song, Min-Ik;Shin, Uk-Seob;Park, Jong-Min
    • The Korean Journal of Pharmacology
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    • v.25 no.1
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    • pp.87-91
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    • 1989
  • Effect of ginseng butanol fractions on the hepatic mitochondrial monoamine oxidase activity with ethanol treatment was investigated in this experiment. Ethanol treatment, either acutely or chronically, increased the hepatic mitochondrial monoamine oxidase activity compared to control group. Whereas, treatment with ginseng butanol fractions lowered the ethaol-induced monoamine oxidase activity. Acetaldehyde, the major metabolite of ethanol, significantly increased the hepatic mitochondrial monoamine oxidase activity more than ethanol did. It was also observed that ginseng butanol fractions reduced the increase of the hepatic mitochondial monoamine oxidase activity by acetaldehyde. From these results, it is suggested that ginseng butanol fractions may be associated with the modulation of the hepatic mitochondrial monoamine oxidase activity in ethanol-treated animals.

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Synthesis of new pyrazoles and their herbicidal effects (새로운 pyrazole 유도체의 합성과 제초활성)

  • Jeon, Dong-Ju;Lee, Jung-No;Kim, Hyung-Rae;Song, Jong-Hwan;Hwang, In-Taek;Ryu, Eung-K.
    • The Korean Journal of Pesticide Science
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    • v.3 no.1
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    • pp.96-101
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    • 1999
  • 3-Trifluoromethylpyrazoles and 4-benzenecarbinolpyrazoles were prepared by the new synthetic methodologies, and their herbicidal effects were tested (in vivo) in the upland conditions and in the flooded paddy conditions for the purpose of the development of new herbicides. In upland conditions, most of the pyrazoles showed weak herbicidal effects at 4 kg/ha dosage in the post-emergence test, while no herbicidal effects in the pre-emergence test. In the flooded paddy conditions, some of the pyrazoles showed good herbicidal effects at a rate of 4 kg/ha, especially, 3-trifluoromethyl-4-(4-methoxybenzoyl)pyrazole showed the best herbicidal activity with good selectivity between rice and weeds. But other derivatives substituted with electron-donating groups such as dior trimethoxy and sulfides, and 4-benzenecarbinolpyrazoles showed weak herbicidal effects.

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Synthesis and SAR of N-Chlorophenyl Substituted Piperrazinylethyl-aminomethylpyrazoles as 5-HT3A Inhibitors

  • Lee, Byung-Hwan;Choi, In-Sung;Rhim, Hye-Whon;Choi, Kyung-Il;Nah, Seung-Yeol;Nam, Ghil-Soo
    • Bulletin of the Korean Chemical Society
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    • v.30 no.11
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    • pp.2707-2712
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    • 2009
  • 5-$HT_{3}$ receptor;5-$HT_{3A}$ receptor channel activity;Novel 5-$HT_{3}$ receptor channel current blockers;Chlorophenyl substituted piperazinylethylaminomethylpyrazoles; The 5-$HT_{3A}$ receptors are one of ligand-gated ion channels and are known to be involved in visceral pain, anxiety, or anticancer agent-induced nausea and vomiting. In present study, we designed novel skeletons based on the developed 5-$HT_{3}$ receptor antagonists and evaluated their effects on 5-$HT_{3A}$ receptor channel currents ($I_{5-HT}$) of a series of pyrazole derivatives having N-chlorophenylpiperazine functionality (6-9). We found that most of N-p-chlorophenyl substituted piperazinyl-pyrazole derivatives (7b, 7c, 7e and 7h) exhibited the high potency for the inhibition of $I_{5-HT}$, whereas the compound without chloride (6) or with m-chlorophenyl group (a serious of 8 and 9) showed the low potency. These result indicate that p-chlorophenyl group is might play an important role for increasing the inhibitory potency on $I_{5-HT}$.