• Bulletin of the Korean Chemical Society
• /
• v.27 no.11
• /
• pp.1861-1864
• /
• 2006

• Journal of Powder Materials
• /
• v.15 no.5
• /
• pp.399-404
• /
• 2008

Spray pyrolysis was applied to prepare $M_{3}MgSi_{2}O_{8}:Eu^{2+}$ (M=Ca, Sr, Ba) blue phosphor powder. The library of a Ca-Sr-Ba ternary system was obtained by a combinatorial method combined with the spray pyrolysis in order to optimize the luminescent property under vacuum ultraviolet (VUV) excitation. 10 potential compositions were chosen from the first screening. The emission shifted to longer wavelength as Ca became a dominant element and the emission intensity was greatly reduced in the composition region at which Ba is dominant element. On the base of the first screening result, the second fine tuning was carried out in order to optimize the luminescence intensity under VUV excitation. The optimal composition for the highest luminescence intensity was $(Ca_{1.7},\;Sr_{0.3},\;Ba_{1.0})Si_{2}O_{8}:Eu^{2+}$ which had the color coordinate of (0.152, 0.072) and about 64% emission intensity of $BaMgAl_{10}O_{17}$ (BAM) phosphor.

• The Korean Journal of Pesticide Science
• /
• v.8 no.1
• /
• pp.8-15
• /
• 2004

A synthesis of new $\beta$-ketoacetoanilide chloride derivatives and anti fungal activity of these compounds library against 6 typical plant pathogens were described. Reaction of ketene dimer with chlorine followed by treatment of aniline derivatives gave 89 kinds of the corresponding $\beta$-ketoacetoanilide chlorides through combinatorial synthetic technology using Carousel Reaction Stations. Evaluation of antifungal activity (in vivo) of this chemical library against rice blast, rice sheath blight, tomato aray mold, tomato late blight, wheat leaf rust and barley powdery mildew was carried out. In general, $\beta$-ketoacetoanilide chlorides which present a substituent at 4 in phenyl group(para) of the compounds showed selective control activity against tomato late blight caused by Phytophthora infestans.

• Journal of the Korean Ceramic Society
• /
• v.41 no.5
• /
• pp.381-387
• /
• 2004

Recently developed Plasma Display Panels (PDP) require phosphors of high luminance at Vacuum Ultraviolet (VUV) excitation. The present investigation developed new PDP phosphors using combinatorial chemistry method. We applied T $b^{3+}$ -activated yttrium gadolinium phosphates system to our combinatorial fine-tuning technique. As a result, the optimum composition was determined to be (G $d_{0.74}$ $Y_{0.11}$T $b_{0.15}$) $P_{1.15}$ $O_{\delta}$ through the two-step combinatorial screening process including excess phosphorous and Gd replacement. We found that the sample of the optimum composition shows a higher luminescence efficiency at VUV excitation and a shorter decay time than the commercially available Z $n_2$ $SiO_4$:Mn phosphor.

• Korean Journal of Materials Research
• /
• v.13 no.12
• /
• pp.785-790
• /
• 2003

We have synthesized some phosphors in the system $CaO-Y_2$$O_3$-$Al_2$$O_3$by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the library was screened from the emission intensities of individual samples under VUV excitation. In $Tb^{ 3＋}$-activated $CaO-Y_2$$O_3$-$Al_2$$O_3$, green phosphors showing good intensity were found to be X$O_3$$O_{7}$, CaYA1O$_4$, YA1O$_3$, $Y_3$$Al_{5}$$O_{12}$, $Y_4$$A1_2$$O_{9}$ .

• Archives of Pharmacal Research
• /
• v.27 no.5
• /
• pp.518-523
• /
• 2004

An allergic reaction ensues after antigen binds to mast cell or basophil high affinity IgE receptor, Fc$\varepsilon$RI, resulting in degranulation of various inflammatory mediators that produce various allergic symptoms. In this study, i) we isolated the active component for the inhibition of mast cell degranulation from the extract of leaves of Castanea crenata and identified it as quercetin; ii) we established the total synthesis procedure of quercetin; iii) using quercetin as positive control, we excavated some lead compounds that possess inhibitory activities for mast cell degranulation by screening the chemical libraries of 1,3-oxazolidine derivatives prepared by solid phase combinatorial chemistry. Some of 1,3-oxazolidine compounds possessing acetyl and 3',4'-dichlorophenyl group displayed strong inhibitory activities on Fc$\varepsilon$RI-mediated mast cell degranulation, suggesting that they can be used as lead compounds for the development of anti-allergic agents.

• 한국정보디스플레이학회:학술대회논문집
• /
• 2004.08a
• /
• pp.650-653
• /
• 2004

We have synthesized some phosphors in the system MO-$Al_2O_3-SiO_2$(M=Sr, Ba) by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the liblary was screened from the emission intensities of individual samples under 365nm excitation. As we were screened the higher luminescent candidate composition (or candidate host lattice) at 365nm excitation, investigated whether good radiation was possible at the 405 or 465nm excitation by give the host lattice to be discovered more various change. From libraries about 2 systems, the compound to be expected in long wavelength among the compound to be screened are $Sr_4Al_{14}O_{25}$, $Sr_3Al_2O_6$, $SrAl_2Si_2O_8$, and $BaAl_2Si_2O_8$.

• 한국정보디스플레이학회:학술대회논문집
• /
• 2003.07a
• /
• pp.836-839
• /
• 2003

We have synthesized some phosphors in the system $CaO-Y_{2}O_3-Al_{2}O_{3}$ by combinatorial polymerized-complex method. Composition and synthetic temperature of phosphors in the liblary was screened from the emission intensities of individual samples under VUV excitation. In $Tb^{3+}$-activated $CaO-Y_{2}O_3-Al_{2}O_{3}$, green phosphors showing good intensity were found to be $CaYAl_{3}O_{7}$, $CaYalO_{4}$, $YAlO_{3}$, $Y_{3}Al_{5}O_{12}$, $Y_{4}Al_{2}O_{9}$, $Ca_{3}Al_{2}O6$.

• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1997.11a
• /
• pp.47-50
• /
• 1997

Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

• Journal of Pharmaceutical Investigation
• /
• v.30 no.3
• /
• pp.191-199
• /
• 2000

Genomics is providing targets faster than we can validate them and combinatorial chemistry is providing new chemical entities faster than we can screen them. Historically, the drug discovery cascade has been established as a sequential process initiated with a potency screening against a selected biological target. In this sequential process, pharmacokinetics was often regarded as a low-throughput activity. Typically, limited pharmacokinetics studies would be conducted prior to acceptance of a compound for safety evaluation and, as a result, compounds often failed to reach a clinical testing due to unfavorable pharmacokinetic characteristics. A new paradigm in drug discovery has emerged in which the entire sample collection is rapidly screened using robotized high-throughput assays at the outset of the program. Higher-throughput pharmacokinetics (HTPK) is being achieved through introduction of new techniques, including automation for sample preparation and new experimental approaches. A number of in vitro and in vivo methods are being developed for the HTPK. In vitro studies, in which many cell lines are used to screen absorption and metabolism, are generally faster than in vivo screening, and, in this sense, in vitro screening is often considered as a real HTPK. Despite the elegance of the in vitro models, however, in vivo screenings are always essential for the final confirmation. Among these in vivo methods, cassette dosing technique, is believed the methods that is applicable in the screening of pharmacokinetics of many compounds at a time. The widespread use of liquid chromatography (LC) interfaced to mass spectrometry (MS) or tandem mass spectrometry (MS/MS) allowed the feasibility of the cassette dosing technique. Another approach to increase the throughput of in vivo screening of pharmacokinetics is to reduce the number of sample analysis. Two common approaches are used for this purpose. First, samples from identical study designs but that contain different drug candidate can be pooled to produce single set of samples, thus, reducing sample to be analyzed. Second, for a single test compound, serial plasma samples can be pooled to produce a single composite sample for analysis. In this review, we validated the issue whether the second method can be applied to practical screening of in vivo pharmacokinetics using data from seven of our previous bioequivalence studies. For a given drug, equally spaced serial plasma samples were pooled to achieve a 'Pooled Concentration' for the drug. An area under the plasma drug concentration-time curve (AUC) was then calculated theoretically using the pooled concentration and the predicted AUC value was statistically compared with the traditionally calculated AUC value. The comparison revealed that the sample pooling method generated reasonably accurate AUC values when compared with those obtained by the traditional approach. It is especially noteworthy that the accuracy was obtained by the analysis of only one sample instead of analyses of a number of samples that necessitates a significant man-power and time. Thus, we propose the sample pooling method as an alternative to in vivo pharmacokinetic approach in the selection potential lead(s) from combinatorial libraries.