• Bulletin of the Korean Chemical Society
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• v.35 no.2
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• pp.617-621
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• 2014

An efficient and selective method for the synthesis of ethyl 2-amino/aryloxy-3-aryl-4-oxo-5-phenyl-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidine-7-carboxylate derivatives has been developed. The main process involved the reaction of diethyl 1-phenyl-3-((triphenylphosphoranylidene)amino)-1H-pyrrole-2,4-dicarboxylate and aromatic isocyanates, followed by addition of amines/phenols in the presence of catalytic amount of sodium ethoxide or solid potassium carbonate.

• Bulletin of the Korean Chemical Society
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• v.26 no.6
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• pp.986-988
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• 2005

• Archives of Pharmacal Research
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• v.13 no.4
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• pp.347-350
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• 1990

The hydrazine derivative 2 has been utilized for the synthesis of three different fused 1, 2, 4-triazolo [4, 3-a] pyrimidine derivatives 4, 5, &6 and a tetrazolo [1, 5-a] pyrimidine derivative 7. Reaction of 2 with the chalcone analogue 2-thenylidene-2'-acetothienone, gave the pyrazoline derivative 8.

• Bulletin of the Korean Chemical Society
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• v.34 no.10
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• pp.3129-3132
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• 2013

• 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.

• Bulletin of the Korean Chemical Society
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• v.25 no.11
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• pp.1631-1632
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• 2004

• Applied Biological Chemistry
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• v.41 no.1
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• pp.99-103
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• 1998

Triazolopyrimidine sulfonanilide (TP) derivative is one of excellent herbicide compounds. We have synthesized three classes of a new sulfonamide derivative (TPP) as Acetolactate synthase (ALS) inhibitors, in which the benzene ring in TP skeleton was converted to substituted pyrimidyl ring and examined their inhibitory activities on barley for ALS. $I_{50}$ values of the inhibitors ranged from 0.005 to 2 mM. Comparing the $I_{50}$ value of each class of TPP derivatives, the substituents in pyrimidine and triazolopyrimidine ring were found to affect the degree of ALS inhibition. TPP with substituted methyl group in pyrimidine ring showed higher inhibitory activity than that with methoxy group, while the substitution of the cyclopentano group in triazolopyrimidine ring gave very large inhibitory activity than that of methyl group. The present study established that variation of the electron density by substitution at heterocyclic ring is a very important factor for ALS inhibition, but showed no dependence on steric effect by substituents.

• Archives of Pharmacal Research
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• v.23 no.2
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• pp.128-138
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• 2000

In continuation of the previous work (Fathalla, 1992) on the synthesis of some heterocycles containing uracil moiety, we report herein the incorporation of uracil moiety into cyan-opyridine thione, thiosemecarbazone, semicarbazone, cyanopyridine, ami nocyano pyridine, isoxazoline, pyrazoline, pyrimidine, triazolo pyrimidine, pyran, selena and thiazole derivatives which might modify their biological activities. The biological studies revealed that the chemical compound III f showed high molluscicdal activity than other compounds. The profile of the nucleoprotein extracted from chemically (compound IIIc, e, f and g) treated or UV-irradiated B.alexandrina snails did not show appreciable differences when compared to non-treated (native) snails by using SDS-PAGE, where no obvious qualitative or quantitative differences were observed. Immunization of experimental animals with the nucleoprotein extracted from native, chemically (compound III f ＆ g) treated or physically treated B.alexandrina snails induced significant protection against challenge with normal S.mansoni cercariae, as compared to the non-immunized challenged control. As well as , a decrease in the number of granuloma formation and the size range of granuloma was also observed in immunized animals. It is concluded that, compounds III f and g have a potent molluscicidal activity. They also induced chemical modification comparable to that induced by physical treatment in the snail's nucleoprotein, which could possibly be used in immunization against S. mansoni infection.

• Bulletin of the Korean Chemical Society
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• v.21 no.3
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• pp.321-327
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• 2000

Polynucleotide analogues containing pyrimidine (uracil and thynime) bases, $poly[(1'{\beta}-uracil-1-yl-2'.5'-dideoxy-D-glycero-pent-4'-enofuranose)-alt-(maleic$ acid)] (12) and $poly[(1'-{\beta}-thymin-1-yl-2'5'-dideoxy-D-glycero-pent-4'-enofuranose)-alt-(maleic$, acid)] (15), were synthesized by the altermating copolymerization of relevant nucleosied derivatives and maleic anhydride, and the subsequent hydrolysis. The polymers had quite similar structures to the natural polymes and were soluble in water, They showed high hypochromicities up to 49% and excimer fluorescence due to the base stacking, and polyelectrolyte behavior. Since the polymers had compact structrures, depyrimidinations, the release of pyrimidine bases from the polymer backbone, occurred in aqueous solutions with higher rates compared with those of the natural polymers.

• 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.