• Applied Biological Chemistry
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• v.39 no.3
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• pp.235-240
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• 1996

The most stable stereo conformer in non substituted benzenesulfonyl urea, 1 was the II-keto form, which the molecule was intramolecular associated(H-bond) coformer between imide group and N atom on the Pyrimidine ring. The hydrolytic degradation of 2 derivatives were proceeds by nucleophilic addition reaction(p<0) with orbital controlled intermolecular interaction between LUMO with electron donating$(\sigma<0)$ groups of 2 and HOMO of water molecule. N-(4,6-disub. pyrimid ine-2-yl)aminocarbonyl-2-(1,1-dimethoxy-2-fluoro)ethylbenze nesulfonamides,3 and N-(4,6-disub. triazine-2-yl)aminocarbonyl-2-(1,1-d imethoxy-2-fluoro)ethylbenzenesulfonamides,4 we re synthesized and their herbicidal activities in vivo against bulrush (Scirpus juncoides.) were measured by the pot test under the paddy conditions And the structure activity relationships(SAR) were analyzed by the multiple regression technique. The results of the SAR suggested that the 3 and 4 derivatives indicated dependent on the hydrophobicity of the 4,6-disubstituents and the heterocyclo group, where the optimal value $((log\;P)_{opt.}=0.89)$ of hydrophobicity was 0.89. The pyrimidine substituents, 3 showed higher herbicidal activity than the triazine substituents, 4. Among them, 4,6-dimethoxypyrimidine substituent, 3a showed the best herbicidal activity.

• Bulletin of the Korean Chemical Society
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• v.26 no.12
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• pp.2021-2026
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• 2005

The oxidation of cytidine 1 and inosine 5 by sodium metaperiodate followed by the reaction of the product with $CH_3I$ in NaOH afforded 2',4'-dihydroxyhexopyranosyl derivatives 2 and 14 respectively. The reaction of thiophene-2-carboxylic acid or furfural with cytidine were taken place via cycloaddition afforded adducts 3 and 4 respectivily. The bromination of inosine 5 or its 2',3'-O-isopropylidine inosine 6 led to the formation of 8-bromoanalogue 7 and 8, respectively. The reaction of 8-bromo-2',3'-O-isopropylidine inosine (8) with ethylglycinate hydrochloride afforded 8-ethoxycarbonylmethylaminoinosine 9. The alkylation of the compound 6 with urea led to the formation of 3-carbonylaminoinosine 10. The oxidation of 6 with DCC afforded 4'-formyl derivative 11, which on reaction with ethyl glycinate hydrochloride followed by reaction with sodium cyanoborohydride afforded 12, while the treatment of dialdehyde inosine 13 with ethyl cyanoacetate in the presence of 0.5 N NaOH afforded compound 15.

• The Korean Journal of Pesticide Science
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• v.9 no.2
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• pp.153-158
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• 2005

Safening activities of optically active ${\alpha}$-methylbenzylphenylureas on crop injury of rice (Oryza sativa L., cv. Tsukinohikari, japonica) caused by bensulfuron-methyl (methyl 2-[[[[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]methyl]benzoate) and pyribenzoxim (benzophenone o-[2,6-bis[(4,6-dimethoxy-2-pyrimidinyl)oxy]benzoyl]oxime) were investigated. Some derivatives of the optically active compounds exhibited strong safening activity against growth inhibition of rice by bensulfuron-methyl. Out of the derivatives tested, (S)-2,3-diCl and (S)-2-F-4-Me derivatives showed greater relieving activity than that of dymuron. In addition, the stress relieving activity was also obtained when they were applied at 4 days after bensulfuron-methyl treatment. On the other hand, crop injury caused by pyribenzoxim was relieved by about 95% with (S)-2-F-4-Me derivative in shoots and roots of rice seedlings.

• Asian-Australasian Journal of Animal Sciences
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• v.12 no.6
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• pp.904-907
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• 1999

The experiment was aimed at studying the effect of ruminal $NH_3-N$ levels on ruminal fermentation, microbial population, urinary purine derivative excretion, digestibility and rice straw intake in swamp buffaloes. Five, 3 to 4 years old, rumen fistulated swamp buffaloes were randomly assigned according to a $5{\times}5$ Latin square design to rceive five different intraruminal infusions of $NH_4HCO_3$ (0, 150, 300, 450 and 600 g/d) on a continuous daily basis. Rice straw as a roughage was offered ad libitum while concentrate was given at 0.8% BW daily. The results were that as levels of $NH_4HCO_3$ increased, ruminal $NH_3-N$ concentrations increased from 7.1 to 34.4 mg%. The highest digestibility and voluntary straw intakes were found at 13.6 to 17.6 mg% ruminal $NH_3-N$ levels; straw intake was highest at 13.6 mg%. Total bacterial and protozoal counts linearly increased as the ruminal $NH_3-N$ increased and were highest at 17.6 mg%. Total urinary purine derivatives and allantoin excretion were highest (44.0, 37.4 mM/d) at 17.6 mg% ruminal $NH_3-N$. Highest total VFAs (115 mM) were obtained a 13.6 mg% ruminal $NH_3-N$ while blood urea nitrogen significantly increased as ruminal $NH_3-N$ increased. The results from this experiment suggest that optimum ruminal $NH_3-N$ in swamp buffaloes is higher than 13.6 mg%, for improving rumen ecology, microbial protein synthesis, digestibility and straw intake.

• Asian-Australasian Journal of Animal Sciences
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• v.19 no.6
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• pp.857-864
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• 2006

The aim of this study was to apply the Cornell net carbohydrate and protein system (CNCPS) in subtropical Taiwan. This was done by means of 3 trials, viz, in situ, lactation and metabolic trials, the latter using the urinary purine derivatives (UPD) to estimate the ruminal microbial yield. Dietary treatments were formulated according to different nutrient requirement systems including, (1) a control NRC78 group on NRC (1978), (2) a NRC88 group on NRC (1988), and (3) a CNCPS group on Cornell Net carbohydrate and protein system model. Results from the lactation trial showed that DM intake (DMI) was higher (p<0.05) in the NRC78 than the other treatment groups. The treatments did not significantly influence milk yield, but milk yield after covariance adjustment for DMI was higher in the CNCPS group (p<0.05). The FCM, milk fat content and yield were greater in both the NRC78 and the NRC88 group over the CNCPS group (p<0.05). The treatments did not significantly influence the DMI adjusted FCM. The solid-non-fat and milk protein contents were higher in the CNCPS group (p<0.05) with or without DMI covariance adjustment. Lactating efficiency was higher in the CNCPS group (p<0.05) compared to the other groups. The significantly lowest milk urea-N (MUN) with better protein utilization efficiency in the CNCPS group (p<0.05) suggested that less N would be excreted into the environment. Cows in the CNCPS group excreted significantly more and the NRC88 group significantly less urinary purine derivatives (UPD) implying that more ruminal microbial protein was synthesized in the CNCPS over the NRC88 group. The CNCPS could become the most useful tool in predicting the trends in milk yield, microbial yield and MUN.

• Journal of the Korean Chemical Society
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• v.58 no.5
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• pp.445-449
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• 2014

A convenient and efficient method has been developed for the one-pot synthesis of dihydropyrimidinones (DHPMs) compounds. Dihydropyrimidinone derivatives were synthesized in good yields using ethyl acetoacetate, aldehyde (aromatic and aliphatic) and urea or thiourea in the presence of ZnO nanoparticles as a catalyst in $H_2O$ as solvent at $80^{\circ}C$. This green chemistry procedure applied to the Biginelli reaction using ZnO nanoparticles as catalyst and illustrated as a rapid preparation of DHPMs in water as solvent. The products were identified by physical data (mp) by comparison with those reported in the literatures.

• Bulletin of the Korean Chemical Society
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• v.34 no.7
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• pp.2011-2015
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• 2013

To improve the water solubility of arylsulfonylimidazolidinone (JSH-2282), a potent anti-cancer agent, two urea derivatives, sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)-phenyl)ureido)succinate (2a) and sodium (S)-2-(3-(4-(5-((S)-2-oxo-4-phenylimidazolidin-1-ylsulfonyl)indoline-1-carbonyl)phenyl)ureido)pentanedioate (2b), were synthesized and studied for solubility and anti-cancer activity.

• Journal of the Korean Chemical Society
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• v.63 no.6
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• pp.435-439
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• 2019

An efficient one pot multicomponent synthesis of pyrimidinone derivatives of Biginelli type is described. 4-amino-6-aryl-pyrimidine-5-carbonitrile molecules were synthesized efficiently via three-component Biginelli-type condensation of aldehyde, malononitrile, and semicarbazone as urea substituent in the presence of a catalytic amount of PEG-400 as green medium under microwave irradiation. The reactions proceeded efficiently in the presence of microwave radiation to afford the desired products in good to excellent yields. Products have been confirmed by IR, and NMR spectral analysis. All the molecules were tested for their antimicrobial activity against E. coli, S. aureus, P. aeruginosa and C. tropicalis. Some of the compounds have shown moderate to good inhibition efficiency against both gram-positive and gram-negative bacteria. The potent activity was observed against the fungal species with minimum inhibition concentration 12.5 ㎍/mL.

• Bulletin of the Korean Chemical Society
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• v.31 no.4
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• pp.863-868
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• 2010

Yttrium(III) acetate hydrate-catalyzed novel synthesis of 3,4-dihydropyrimidin-2(1H)-(thio)one derivatives was achieved through one-pot three-component condensation of diversified aldehydes, $\beta$-ketoesters and urea or N-methylurea or thiourea with a molar ratio of 1:1:1.4. In comparison to the classical Biginelli approach, this catalytic method has the advantages of short reaction time and improved product yield.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.184-188
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• 1999

A series of 4-amino Capsaincin anallogs 15, 17 and 19 were prepared to investigate the bioisosteric effect of 4-amino group, and all these compounds exhibited moderate or weak potency from their analgesic test. From our previous results and others, 4-hydroxyl group as well as 3-methoxy substituent could be crucial for high analgesic activity. This biological results also shows that the activity is sensitive to alkyl chain length in hydrophobic region and the phenylacetic amides 19 are more active than the corresponding urea derivatives 17.