• 한국식물생명공학회:학술대회논문집
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• 한국식물생명공학회 2004년도 생명공학 실용화를 위한 비젼
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• pp.29-34
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• 2004

Reduction in stratospheric ozone layer increases the amount of ultraviolet-B radiation (UVB: 280-320 nm) that reaches the earth ’ s surface. UVB radiationcan damage plants, resulting in decrease in growth and productivity. UVB-augmentation studies have indicated that the sensitivity to UVB radiation in plants varies among the species and cultivars. However. there are no definitive answers for the mechanisms of UVB-resistance in higher plants and for bioengineering design and development of UVB-tolerant plants. We have been studying physiological and biochemical aspects of the effects of UVB radiation on growth and yield of rice COryza sativa LJ. aiming to clarify the mechanism of resistance to UVB radiationin rice. At this meeting. weintroduce our research as followed: (1) supplementary UVB radiation has inhibitory effects on the growth. yield and grain development of rice; (2) UVB sensitivity of rice varies widely among cultivars; (3) among Japanese rice cultivars. Sasanishiki. a leading variety in northeast Japan. is more resistant to UVB. while Norin 1. a progenitor of Sasanishiki. is less resistant; (4)UV-sensitive Norin 1 cultivar is deficient in photorepair of UVB-induced cyclobutane pyrimidine dimer (CPD). and this deficiency results from one amino acid residue alteration of CPD photolyase. These results suggest that spontaneously occurring mutation in CPD photolyase gene could lead to difference in UVB sensitivity in rice. and that CPD photolyase might be a useful target for improving UVB-sensitivity in rice by selective breeding or bioengineering of UVB-tolerant rice.

• 미생물학회지
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• 제27권2호
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• pp.139-146
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• 1989

담수상태의 논토양에 처리한 유기인계 살충제 diazinon의분해기작과 그 분해산물에 대하여 조사하였다. 항온조건($30^{\circ}C$)하에서 살균토양에 비하여 비살균토양에서의 diazinon 분해가 보다 빠르게 일어남으로써 담수토양내 diazinon 분해에 미생물의 대사활동이 매우 종요한 것으로 나타났는데, 비살균토양내 diazinon의 반감기는 약 2일이엇고 항온반응 7일만에 95% 이상의 분해가 이루어졌다. 또한 diazinon 분해기간 중 미생물 개체수와 아울러 토양내 monoxygenase 및 esterase 활성의 증가가 이루어졌으며 이는 토양내 diazinon 처리가 이 약제의 분해와 관련된 미생물학적 요인의 생장 또는 활성을 촉진시키고 있음을 보여준다. 이와 관련하여 담수토양내 diazinon 분해산물로서 esterase 작용에 의한 2-isopropyl-6-methyl-4-hydroxy pyrimidine 이외에 monooxygenase에 의한 diazoxon과 hydroxydiazinon, 그리고 sulfotep 등이 mass spectrometry에 의하여 확인되었다.

• Archives of Pharmacal Research
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• 제23권2호
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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.

• Archives of Pharmacal Research
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• 제28권11호
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• pp.1205-1212
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• 2005

2-Thiouracil-5-sulphonic acid N-(4-acetylphenyl) Amide (1) was reacted with a series of aromatic aldehydes giving chalcones 2 (Claisen-Schemidt reaction), some of these chalcones were reacted with urea and thiourea giving pyrimidine-2-one and pyrimidine-2 thione derivatives respectively of the type 3a,b and 4a,b. In addition many chalcones were reacted with hydroxylamine hydrochloride giving isoxazoline derivatives 5a,b. They could also reacted with phenylhydrazine to give pyrazoline derivatives 5a,b, chalcones also were reacted withethylcyano acetate and/or malononitryl in pyridine giving pyran derivatives 7a,c and 8a,c. In another pathway chalcones were epoxidised by $H_{2}O_{2}$ giving epoxides 9a,c which in turn were reacted with phenylhydrazine giving 4-hydroxypyrazoline derivatives 10a,c. In another reaction chalcones were reacted with ethylcyanoacetate in presence of amm.acetate giving pyridone derivatives 11a,d which could be prepared also in exellent yield from compound 1 by its reaction with certain aromatic aldehydes and ethylcyanoacetate in presence of ammonium acetate. Finally, compound 1 was reacted with semicarbazide giving semicarbazone intermediate 12 which in turn was reacted with thionyl chloride giving thiadiazole derivative 13. The biological effects of some of the new synthesized compounds were also investigated.

• 대한화학회지
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• 제55권6호
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• pp.940-951
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• 2011

Reaction of 1-methylpyrimidine-(1H,3H,5H)-2,4,6-trione (1-MBA 1) as an unsymmetrical barbituric acid with cyanogen bromide and various aldehydes in the presence of triethylamine and/or pyridine afforded diastereomeric mixtures of new class of heterocyclic stable 5-aryl-1,1'-dimethyl- and 5-aryl-3,1'-dimethyl-1H,1'H-spiro[furo[2,3-d]pyrimidine-6,5'-pyrimidine]2,2',4,4',6'(3H,3'H,5H)-pentaones which are dimeric forms of 1-methyl barbiturate at the range of $0^{\circ}C$ to room temperature. In the reaction of some aldehydes with 1-MBA and BrCN were afforded a mixture of diastereomers. Another two aldehydes such as 4-cyano- and 2-hydroxybenzaldehydes gave exclusively two diastereomers in which binded to the salt of triethylammonium hydrobromide by intermolecular H-bond in ratio of 1:1. 4-Hydroxybenzaldehyde and 2-pyridinecarbaldehyde gave exclusively one diastereomer under the same condition. Aldehydes possessing strong electron-donor were produced exclusively two geometric isomers of Knoevenagel adduct (E- and Z-isomers). The structures of compounds were deduced by $^1H$ NMR, $^{13}C$ NMR and FT-IR spectroscopy. Mechanism of the formation is discussed.

• 대한화학회지
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• 제53권6호
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• pp.731-741
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• 2009

$NaHSO_4.SiO_2$ 촉매를 이용한 microwave 및 무수조건하에서 새로운 morpholino pyrimidines의 One-pot합성이다. 합성된 모든 화합물을 이용하여 in vitro에서 임상학적인 단리된 박테리아 품종 즉 Bacillus subtilis, Bacillus cerues, Micrococcus luteus , Salmonella typhii에 대해 항균성을 살펴보았고, 균품종 즉 Aspergillus niger, Candida 6, Candida 51에 대해 항진균성을 살펴보았다. 미생물 결과에 대한 합성된 화합물의 구조적 활동성의 관련성에 대해 토론하였다.

• Archives of Pharmacal Research
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• 제24권4호
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• pp.270-275
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• 2001

Bioisostere approach has been shown to be useful to augment potency or to modify certain physiological properties of a lead compound. Based upon well documented bioisosterism, an isosteric replacement of benzene ring of 4-hydroxy-2-quinolone compound (L-695902) with a thiophene moiety was carried out to prepare the title compounds, 4-hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidines 15. The resulting bioisosteric compounds 15 were evaluated for their antagonistic activity (birding assay) for NMDA receptor glycine site.

• Journal of Pharmaceutical Investigation
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• 제30권2호
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• pp.113-118
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• 2000

In order to assay the efficacy of newly synthesized antiviral compounds, pyrimidine analogs, pharmacokinetics of those were established as compared with already marketed zidovudine. Zidovudine (15, 20, 25 and 35 mg/kg), LJ142 (18.52 mg/kg) and LJ143 (15, 18.52 and 30 mg/kg) were administered orally and intravenously in rats, blood samples were collected post-injection(i.e., for 360 min) at appropriate time intervals. Those were analyzed by HPLC with UV detection at 265 nm. Pharmacokinetic parameters $(C_{max},\;T_{1/2},\;MRT,\;AUC,\;AUMC,\;Vd_{SS},\;Cl_t)$ were calculated. AUCs of zidovudine and LJ143 following I.V. dosing of $15{\sim}25\;mg/kg\;and\;15{\sim}18.18\;mg/kg$ were dose-independent. However, AUCs of zidovudine and LJ43 following I.V. dosing of $25{\sim}35\;mg/kg\;and\;18.18{\sim}30\;mg/kg$ were dose-dependent. The relative bioavailability of zidovudine, LJ142 and LJ143 following oral administration were 61.94, 46.44 and 78.24%, respectively.

• 농약과학회지
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• 제5권2호
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• pp.33-36
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• 2001

2-Chloromethyl-1,3-dioxolane기가 치환된 새로운 thiophene sulfonylurea계 유도체들을 합성하였고, 신규 합성된 화합물을 발아전 토양처리와 발아후 경엽처리를 통하여 문제잡초 9종의 제초활성을 규명하였으며, 답작 조건의 이앙벼 및 주요 잡초에 대한 제초활성도 시험하였다. 이 화합물들의 제초활성은 헤테로고리의 치환기에 따라 매우 다르게 나타났는데, 4, 6 위치에 각각 dimethoxy, 혹은 methyl, methoxy가 치환된 pyrimidine, 혹은 triazine이 붙어있는 sulfonylurea들이 활성이 좋았다. 그러나 이들은 2-fluoromethyl-1,3-dioxolane기가 치환된 thiophene sulfonylurea계 유도체보다 일반적으로 제초활성이 약하게 나타났다.

• 한국자기공명학회논문지
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• 제21권2호
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• pp.50-54
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• 2017

Cupin-superfamily proteins represent the most functionally diverse groups of proteins and include a huge number of functionally uncharacterized proteins. Recently, YaiE, a cupin protein from Escherichia coli has been suggested to be involved in a novel activity of pyrimidine/purine nucleoside phosphorylase (PPNP). In the present study, we achieved a complete backbone NMR assignments of YaiE, by a series of heteronuclear multidimensional NMR experiments on its [$^{13}C/^{15}N$]-enriched sample. Subsequently, secondary structure analysis using the assigned chemical shift values identified 10 obvious ${\beta}-strands$ and a tentative $3_{10}-helix$. Taken all together, the results constitute the first structural characterization of a putative PPNP cupin protein.