• Archives of Pharmacal Research
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• v.13 no.4
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• pp.310-313
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• 1990

Hantzsch synthesis of 5-formyluracil (1) methyl acetoacetate (2) and methyl 3-aminocrotonate (3) gave 2, 6-dimethyl-4-(2, 4-dioxo-5-pyrimidy)-1, 4-dihydropyridine-3, 5-dicarboxylic acid dimethylester (4a) in 54.6 yield. As the same procedure, 1, 3-dimethyl-5-formyl-uracil (6) gave 2, 6-dimethyl-4-(1, 3-dimethyl-2, 4-dioxo-5-pyrimidyl)-1, 4-dihydropyridine-3, 5-dicarboxylic acid dimethyl easter (7a) IN 52.2% yield. 4a was methylated to afford 7a also in 52% yield.

• Korean Journal of Environmental Agriculture
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• v.42 no.4
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• pp.389-395
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• 2023

This study evaluated the effects of gibberellic acid (GA₃) on the growth and quality of creeping bentgrass (Agrostis palustris Huds.). Experimental treatments included a No application of fertilizer and GA₃ (NFG) Control [3 N active ingredient (a.i.) g/m²], 0.3GA₃ (GA₃ 0.3 a.i. mg/m²/200 mL), 0.6GA₃ (GA₃ 0.6 a.i. mg/m²/200 mL), 1.2GA₃ (GA₃ 1.2 a.i. mg/m²/200 mL), and 2.4GA₃ (GA₃ 2.4 a.i. mg/m²/200 mL). Additionally, the study included a 1.5N+GA₃ experiment with similar GA₃ treatments combined with 1.5N a.i. g/m² : NFG, Control (3N a.i. g/m²), 1.5N+ 0.3GA₃ (1.5N a.i. g/m²+GA₃ 0.3 a.i. mg/m²/200 mL), 1.5N+0.6GA₃ (1.5N a.i. g/m²+GA₃ 0.6 a.i. mg/m²/200 mL), 1.5N+1.2GA₃ (1.5N a.i. g/m²+GA₃ 1.2 a.i. mg/m²/ 200 mL), and 1.5N+2.4GA₃ (1.5N a.i. g/m²+GA₃ 2.4 a.i. mg/m²/200 mL). Compared to the NFG, turf color index chlorophyll content was not significantly different (p< 0.05). However, shoot length in 1.2GA₃, 2.4GA₃, 1.5N+0.3GA₃, 1.5N+0.6GA₃, 1.5N+1.2GA₃, and 1.5N+2.4GA₃ treatments increased by 0.8%, 10.6%, 5.15%, 8.3%, 13.5 %, and 21.6%, respectively, compared to the control. As compared to the control, clipping yield in 1.5N+1.2GA₃ and 1.5N+2.4GA₃ treatments increased by 7.1% and 14.3 %, respectively. These results indicated that GA₃ application increased shoot length, with the 1.2GA₃ treatment showing shoot length similar to the control (3N a.i. g /m² ).

• Archives of Pharmacal Research
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• v.21 no.2
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• pp.174-178
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• 1998

As a new colon-specific prodrug of 5-aminosalicylic acid (5-ASA), 5-aminosalicyl-glycine (5-ASA-Gly) was prepared by a simple synthetic route in good yield. Apparent partition coefficients of 5-ASA-Gly were lower than those of 5-ASA, which determined in$ CHCl_{3}$/pH 6.8 buffer or n-octanol/pH 6.8 buffer system. Stability of 5-ASA-Gly by peptidases was investigated by incubation of 5-ASA-Gly with the homogenates of tissue and contents of stomach, proximal small intestine or distal small intestine of rats at $37^{\circ}C$. 5-ASA was not detected, indicating that the prodrug was stable in the upper intestine. The amount of 5-ASA liberated from incubation of the prodrug in cecal or colonic contents of rats was about 65% or 27% in 8 hrs, respectively, which indicated that the prodrug activation took place more readily in the rat cecum whose bacterial counts are high like human colon. Results from in vitro experiments suggested 5-ASA-Gly as a promising candidate of a colon-specific prodrug of 5-ASA.

• Bulletin of the Korean Mathematical Society
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• v.45 no.3
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• pp.457-466
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• 2008

Let R be a right near-ring. An R-group of type-5/2 which is a natural generalization of an irreducible (ring) module is introduced in near-rings. An R-group of type-5/2 is an R-group of type-2 and an R-group of type-3 is an R-group of type-5/2. Using it $J_{5/2}$, the Jacobson radical of type-5/2, is introduced in near-rings and it is observed that $J_2(R){\subseteq}J_{5/2}(R){\subseteq}J_3(R)$. It is shown that $J_{5/2}$ is an ideal-hereditary Kurosh-Amitsur radical (KA-radical) in the class of all zero-symmetric near-rings. But $J_{5/2}$ is not a KA-radical in the class of all near-rings. By introducing an R-group of type-(5/2)(0) it is shown that $J_{(5/2)(0)}$, the corresponding Jacobson radical of type-(5/2)(0), is a KA-radical in the class of all near-rings which extends the radical $J_{5/2}$ of zero-symmetric near-rings to the class of all near-rings.

• The Korean Journal of Physiology and Pharmacology
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• v.21 no.2
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• pp.169-177
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• 2017

Lamotrigine is an antiepileptic drug widely used to treat epileptic seizures. Using whole-cell voltage clamp recordings in combination with a fast drug application approach, we investigated the effects of lamotrigine on 5-hydroxytryptamine $(5-HT)_3$ receptors in NCB-20 neuroblastoma cells. Co-application of lamotrigine ($1{\sim}300{\mu}M$) resulted in a concentration-dependent reduction in peak amplitude of currents induced by $3{\mu}m$ of 5-HT for an $IC_{50}$ value of $28.2{\pm}3.6{\mu}M$ with a Hill coefficient of $1.2{\pm}0.1$. These peak amplitude decreases were accompanied by the rise slope reduction. In addition, $5-HT_3$-mediated currents evoked by 1 mM dopamine, a partial $5-HT_3$ receptor agonist, were inhibited by lamotrigine co-application. The $EC_{50}$ of 5-HT for $5-HT_3$ receptor currents were shifted to the right by co-application of lamotrigine without a significant change of maximal effect. Currents activated by 5-HT and lamotrigine co-application in the presence of 1 min pretreatment of lamotrigine were similar to those activated by 5-HT and lamotrigine co-application alone. Moreover, subsequent application of lamotrigine in the presence of 5-HT and 5-hydroxyindole, known to attenuate $5-HT_3$ receptor desensitization, inhibited $5-HT_3$ receptor currents in a concentration-dependent manner. The deactivation of $5-HT_3$ receptor was delayed by washing with an external solution containing lamotrigine. Lamotrigine accelerated the desensitization process of $5-HT_3$ receptors. There was no voltage-dependency in the inhibitory effects of lamotrigine on the $5-HT_3$ receptor currents. These results indicate that lamotrigine inhibits $5-HT_3$-activated currents in a competitive manner by binding to the open state of the channels and blocking channel activation or accelerating receptor desensitization.

• Journal of the Korean Chemical Society
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• v.52 no.3
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• pp.249-256
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• 2008

3-Acetyl/Formyl 4-hydroxy-2H(1)-benzopyran-2-one on treatment with malonitrile and ethyl cyanoacetate yielded 1,1-dicyano-2-[4/-hydroxy-2/H(1)-benzopyran-2/-one-3/-yl] ethene/propene 2a-h and ethyl-2-cyano-3-[4/-hydroxy-2/H (1)-benzopyran-2/-one-3/-yl] propenoate/butenoate 3a-h respectively. The 1,3 dipolar reaction of 2a-h with NaN3 gave the tetrazole derivative 4a-h. 3a-h on cyclization with PPA gave 3-cyano-2H,5H-pyrano [3, 2-c] benzopyran-2,5-diones 5a-h which on 1,3 dipolar reaction with NaN3 to gave 3-(1/H-tetrazol-5/-yl)-2H,5H-pyrano[3, 2-c] benzopyran-2,5-diones 6a-h. The structures of the compounds have been established on the basis of the spectral and analytical data. All the compounds were screened for their antimicrobial activities and have been found to exhibited significant antibacterial activities. Compounds 2h and 4h showed the activity 50g/mL.

• Microbiology and Biotechnology Letters
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• v.51 no.1
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• pp.37-42
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• 2023

Neutral and non-essential amino acid, glutamine (Gln), plays an essential role in supplying nitrogen to all the amino acids and nucleotides in the mammalian body. Gln is also the most important carbon source that provides intermediates for gluconeogenesis and fatty acid synthesis and supplements the tricarboxylic acid cycle in fast-growing cancer cells. Among the known 14 Gln transporter genes, soluted carrier family 1 member 5 (SLC1A5) has been reported to be closely associated with cancer cell growth. Three variants (v1, v2, and v3) have been derived from SLC1A5. Here, we established a heterologous gene expression system for the active form of human SLC1A5 variant-2 (hSLC1A5v2) in Escherichia coli. v2 is the smallest variant that has not yet been studied. Four expression systems were investigated: pBAD, pCold, pET, and pQE. We also addressed the problem of codon usage bias. Although pCold and pET overexpressed hSLC1A5v2 in E. coli, they were functionally inactive. hSLC1A5v2 using the pBAD system was able to catalyze the successful transport of Gln, even if it was not highly expressed. Initial activity of hSLC1A5v2 for [¹⁴C] Gln uptake in E. coli reached up to 6.73 μmole·min^-1·gDW^-1 when the cell was induced with 80 mM L-arabinose. In this study, we demonstrated a heterologous expression system for the human membrane protein, SLC1A5, in E. coli. Our results can be used for the functional comparison of SLC1A5 variants (v1, v2, and v3) in future studies, to facilitae the developement of SLC1A5 inhibitors as effective anticancer drugs.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.93-96
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• 1982

By using recemic 3-bromo-5-isobutyl-5-methylhydantoin (3a') in dry N, N-dimethylformamide which is a model reagent for asymmetric bromolactonization, bromolactonization of a series of olefinic acids was carried out to furnish corresponding bromolactones in moderate yields.

• Journal of the Korean Chemical Society
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• v.43 no.4
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• pp.447-455
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• 1999

Allyl (5R)-(Z)- and (5R)-(E)-6-[(2S)-2,3-isopropylidenedioxypropylidene]Penicillanate(10a and 10b) were prepared from allyl (5R)-dibromopenicillanate(6) via a sequence of reactions involving condensation with 2,3-O-isopropylidene-D-glyceraldehyde, reduction with $Zn-NH_4OAc$, and Mitsunobu elimination. Deprotection of isopropylidene and allyl groups of 10a gave potassium (5R)-(Z)-6-[(2S)-2,3-dihydroxypropylidene]penicillanate(4). However, deprotection of isopropylidene group of 10b afforded ${\alpha},\;{\beta}$-unsaturated-lactone(12). Allyl (5R)-(Z)- and (5R)-(E)-6-[(2S)-2-(t-butyldimethlsilyloxy)propylidene]penicillanate(18a and 18b) were prepared from ally (5R)-dibromopenicillanate(6) via a sequence of reactions involving condensation with (2S)-2-(t-butyldimethylsilyloxy)propanal(15), reduction with $Zn-NH_4OAc$ and Mitsunobu elimination or mesylation-elimination. Deprotection of t-butyldimethylsilyl and allyl groups of 18a and 18b gave potassium (5R)-(Z)- and (5R)-(E)-6-[(2S)-2-hydroxypropylidene]penicillanate(5a and 5b), respectively.

• KOREAN JOURNAL OF CROP SCIENCE
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• v.7 no.1
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• pp.65-70
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• 1969

These studies were carried to clarify the application effect of high leveled superphosphate fertilizer and the effect to the yield and growth of rice by the application of composts enriched with superphosphate fertilizer and the results were as follows: 1) Neither statistical significance was convinced between the yield and yield component factor in each treatment in the terms of superphosphate effects, nor the additional application effect of superphosphate fertilizer was appeared. 2) In the terms of grain yield, the statistical significance was not revealed in the plots of composts applied 1000kg per 10a, of superphosphate applied 5kg, 7.5kg and 10kg per 10 a, but grain yield were 220kg in the plot of composts applied 1000 kg per 10 a, 232kg in the plot of superphosphate applied 5 kg per 10 a, 266kg in superphosphate applied 7.5 per 10a, and 243kg of 10kg $P_2O_5$ per 10a. 3) The methods of applying superphosphate and composts to rice plant making composts enriched with superphosphate fertilizer a few monath before the basal application were recommended to increase grain yield and each factor of grain component. 4) The interaction of applying composts and superphosphate was revealed that applying composts with the $P_2O_5$ was recommended. 5) Grain yields were higher in the plots of 1, 000kg of composts enriched with 7.5kg of $P_2O_5$ per 10 a, and 1, 000kg of composts with 5kg of $P_2O_5$ per 10 a other than the rest of 10 treatments. 6) Appyling composts in the test was convinced as effective results to accelerate the maturing rate.