• YAKHAK HOEJI
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• v.46 no.2
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• pp.89-92
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• 2002

Allylthio group of the sulfur compounds of garlic oil plays an important role for prevention and treatment of hepatic diseases induced by toxic substances or carbon tetrachloride. Thus allylthio group as pharmacologically active group was introduced into pyridazine heterocycle ring. Aryloxyallylthiopyridazine derivatives were synthesized and their hepatoprotective activities were screened in rat. The activities of these compounds were weaker than alkoxyallylthiopyridazine derivatives, which exhibit a superior hepatoprotective effect.

• Archives of Pharmacal Research
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• v.17 no.6
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• pp.411-414
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• 1994

Phenylazocyanothioacetamide 1 reacts with malononitrile to afford the pyridinethione 4 which reacts with phenacylbromide to yield the pyridine-S-phenacyl derivative 6, 1 reacts with ethyl cyanoacetate to yield the pyridazine derivative, 8, and with phenacyl bromide to afford the N-phenacyl derivative 11, instead of the thiazole 10. Compound 11 afforded the pyrazolopyridine 13 on reaction with malononitrile while 10 was obtained on coupling of the thiazole 14 with diazotised aniline. Compound 10 reacts with malononitrile to afford the thizaolyl pyridazine 15. Compound 1 reacts with malononitrile dimer to afford the pyriodopyridazine derivative 17a. 1 reacts also with active methylene heterocycies to afford the pyrazolo and thiazolo-fused phridazines 20 and 23 respectively.

• Journal of Integrative Natural Science
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• v.11 no.2
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• pp.107-112
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• 2018

p38 MAP kinase belongs to the Mitogen-activated protein (MAP) kinase family; a serine/threonine kinase. It plays an important role in intracellular signal transduction pathways. It is associated with the development and progression of various cancer types making it a crucial drug target. Present study involves the HQSAR analysis of recently reported imidazo[1,2-b]pyridazine derivatives as p38 MAP kinase antagonists. The model was generated with Atom (A), bond (B), chirality (Ch), and hydrogen (H) parameters and with different set of atom counts to improve the model. An acceptable HQSAR model ($q^2=0.522$, SDEP=0.479, NOC=5, $r^2=0.703$, SEE=0.378, BHL=97) was developed which exhibits good predictive ability. A contribution map for the most active compound (compound 17) illustrated that hydrogen and nitrogen atoms in the ring A and ring B, as well as nitrogen atom in ring C and the hydrogen atom in the ring D provided positive activity in inhibitory effect while, the least active compound (compound 05) possessed negative contribution to inhibitory effect. Hence, analysis of produced HQSAR model can provide insights in the designing potent and selective p38 MAP kinase antagonists.

• The Korean Journal of Pesticide Science
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• v.4 no.1
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• pp.32-37
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• 2000

A series of transition metal complexes of 3,6-bis(6'-methyl-2'-pyridyl)pyridazine ($L^{1}$) and 3,6-bis(2'-pyridyl)pyridazine ($L^{2}$) as artificial nuclease, $1{\sim}8$ were synthesized. After determining of X-ray crystal structure, hydrolysis rate constants of phosphates, as DNA model compound and biological activities were confirmed. $L^{2}$-Zn(II) complex, 8 was shown the best hydrolysis rate constant. The $L^{2}$-Ni(II) complex, 5 and $L^{2}$-Co(II) complex, 6 showed the highest herbicidal activity against SCP (Scriptus Juncoids) with excellent tolerance to rice, ORY (Oryzae sativa L.). And the $L^{1}$-Co(II) complex, 2, $L^{1}$-Zn(II) complex, 4 and ligand ($L^{1}$ amp; $L^{2}$) displayed above 90% fungicidal activity against MAG (Magnaporthe grisea).

• Bulletin of the Korean Chemical Society
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• v.10 no.6
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• pp.614-617
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• 1989

• Bulletin of the Korean Chemical Society
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• v.10 no.3
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• pp.317-319
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• 1989

• Journal of the Korean Chemical Society
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• v.58 no.4
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• pp.377-380
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• 2014

A noval derivatives of 3-substituted[1,2,4]triazolo[4,3-b]pyridazine (4a-4o) and 7,8,9,10-tetrahydrobenzo[4,5] thieno[2,3-d][1,2,4]triazolo[4,3-b]pyridazine (7a-7l) is prepared by the reaction of heteroaryl hydrazone from the aldehyde and pyridazinohydrazine derivative, followed by subjecting the intermediate directly to oxidative cyclization employing the mixture of $Me_4NBr$ and Oxone. These derivatives were subjected to preliminary antimicrobial activities against microorganism. All these compounds exhibit good to moderate activity.

• Bulletin of the Korean Chemical Society
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• v.35 no.3
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• pp.721-724
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• 2014

We have explored the potential energy surface for the dissociation of the pyridazine molecular ion using G3 model calculations. The pathways have been obtained for the formation of five possible $C_4H_4^{+{\bullet}}$ isomers by the loss of $N_2$ and the consecutive $H^{\bullet}$ loss. It is predicted that the methylenecyclopropene radical cation is the predominant product in the loss of $N_2$, which is formed via the allenylcarbene radical cation, and $CH_2=C-C{\equiv}CH^+$ is the predominant product in the consecutive $H^{\bullet}$ loss.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.198-200
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• 1990

3, 4-Diphenyl-5-cyanopyridazin-6-one 3 was prepared from the reaction of cyano acetamide 2 with benzihydrazone in dry pyridine. A series of its derivatives was prepard. Tolyl and benene sulphonyl derivatives 6a and 6b are also prepared. 3, 4-Diphenyl-5-cyanopyridazin-6-thione 5 was obtained from 3 by the action of $P_2S_5$ while 3, 4 diphenyl-5-cyano 6-chloropyridazine 4 was obtained from 3 by the action POCl$_3$. The reaction of 4 with hydrazine hydrate directly afforded the pyrazolopyridazine derivative 7. Compound 4 also reacted with phenylhydrazine, aniline, thiophenol and anthranilic acid to yield pyridazine derivatives 8, 9, 10 and 11, respectively. On treatment of compound 11 with acetic anhydride it cyclised to afford pyridazino pyrimidine derivatives 12.

• YAKHAK HOEJI
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• v.58 no.6
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• pp.371-377
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• 2014

A new series of 3-alkylthio-6-allylthio-4(or 5)-methylpyridazines (6a-e)-(7a-e) was synthesized from citraconic anhydride (1) for development of candidates possessing anticancer activity. The process involves the formation of pyridazine ring, dichlorination, monoallythiolation, and further another alkylthiolation. Compounds 6a-e, and 7a-e were prepared from 6-allylthio-3-chloro-4-methylpyridazine (4) or 6-allylthio-3-chloro-5-methylpyridazine (5) via nucleophilic substitution reaction with alkylthiol anion as nucleophile. Intermediates 4, and 5 could be converted to target pyridazines 6a-e, and 7a-e using 1~1.5 equivalent of alkylthiol at reflux temperature in methanol in the presence of sodium hydroxide. The structures of the synthetic compounds were characterized using NMR, IR, and GC-MS analyses.