• 약학회지
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• 제48권4호
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• pp.254-260
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• 2004

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 2,4-difluorophenyl( 2a-5a), 2,5-difluorophenyl(2b-5b), 4-ethylphenyl(2c-5c), 2-hydroxyphenyl(2d-5d) and 2-methylnaphthyl(2e-5e) instead of naphthyl group with hydrogen(3a-3e), methyl(4a-4e), and ethyl(5a-5e) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds( 3a, 4a, 5a, 3d, 4d, 4d, 5d, 3e, and 4e) showed significant anti-fungal activity against T. mentagroPhytes. (E)-N-(3-Phenyl-2-propenyl)-2- hydroxy-benzenemethaneamine( 3d) displayed moderate antifungal activity against all five different fungi.

• 약학회지
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• 제47권5호
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• pp.293-299
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• 2003

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 4-fluorophenyl(2a-5a), 2-fluorophenyl(2b-5b), 2,4-dichlorophenyl(2c-5c), 2,6-dichlorophenyl(2d-5d), 4-nitrophenyl(2e-5e), and 2,3-dihydro-benzo[1,4]dioxan-6-yl( 2f-5f) instead of naphthyl group with hydrogen(3a-3f), methyl(4a-4f), and ethyl(5a-5f) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds(3a, 5a, 3c, 4c, 4d, 5d, 5e, and 4f) showed significant antifungal activity against T. mentagrophytes. (E)-N-Ethyl-(3-phenyl-2-propenyl)-4-nitro-benzenemethaneamine(5e) displayed moderate antifungal activity against all five different fungi.

• 미생물학회지
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• 제33권4호
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• pp.237-241
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• 1997

Streptomyces coelicolor A3(2) 배양액의 lipase(EC 3.1.1.3)는 ${\alpha}$-naphthyl-butyrate에 대하여 활성을 나타내어 ${\alpha}$-naphthyl-acetate에 활성을 나타내는 esterase와 구분할 수 있었다. Streptomyces coelicolor A3(2) 세포외 lipase를 Sephadex G-100, DEAE-Cellulose 그리고 Phenyl-Sepharose CL4B 크로마토그래피의 과정을 통해 16% 수율로 15배 분리정제 하였다. SDS-폴리아크릴아마이드 겔 전기영동에서는 34.7 kDa정도의 분자량을 갖는 것으로 나타났다. Tributyrin를 기질로 사용하였을 때 이 lipase의 최적활성조건은 pH 8에서 9 그리고 $37^{\circ}C$였다. 기질로서 triacylglycerol의 지방산 길이가 증가할수록 활성은 감소하였다. A-factor에 의해 lipase활성이 억제되므로 배양초기의 낮은 lipase활성과 관련될 것으로 보인다.

• Archives of Pharmacal Research
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• 제16권3호
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• pp.219-226
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• 1993

For the analysis of structure relationship of ar-turmerone analogues, the compounds containing the various substituents on the phenyl ring and 1(or 2)-naphthyl group in the place of phenyl of ar-turmerone were prepared and tested their cytotoxicity against HL-60, K-562, and L1210 leukemia cells in vitro. The substituents at para position are methoxy, phenoxy, methyl, trifluoromethyl, fluoro, and chloro. At meta position methoxy, methyl, trifluoromethyl, or chloro groups at ortho position mathoxy or chloro group were introduced. Against HL-60 and K-562 cells, $ED_{50}$ values of the analogues are ranged from 0.8 to $30.0\;\mu{g/ml}$. Againste L1210 cell, these are located more than $20.0\;\mu{g/ml}$. However, 5-carbone-thoxy-2-methyl-6(1-naphthyl)-2-octen-4-one (5n)possesses $ED_{50}$ valuses 0.8, 2.1, $6.5\;\mu{g/ml}$ against HL-60, L1210 cells, respectively. The electronic nature of the substituents on phenyl ring of ar-tumerone dose not affect the biological activity. Therefore the flat structure of aromatic potion of ar-tumerone analogues is the more important factor for their activity rather than its electronic nature. The potentiation of the cytotoxicity with the enlargement of aromatic ring region also supports the importance of the plane structure of this area. The restriction of the single bond rotation between C-6 and aromatic ring through the introduction of substituents at the ortho position of phenyl ring and the increment of size of alkyl group at C-6 position enhances the activity. Therefore the effective conformation should by the one having the orthogonal arrangement between the aromatic ring and the side chain.

• 대한화학회지
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• 제40권5호
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• pp.365-373
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• 1996

Diethylenedisiloxyl 유연격자를 갖는 일련의 새로운 액정화합물을 합성하여 이들의 액정특성 및 말단의 페닐기에 para 치환기들의 스멕틱 그룹 효율성을 조사하였다. 또 말단그룹의 크기 영향을 알아보기 위하여 para 치환된 페닐 대신 $\beta$-naphthyl 그룹을 도입한 화합물도 아울러 합성하였다. 모든 화합물들은 85-95%의 높은 수율로 합성되었으며, 합성된 화합물들은 모두 양방성 액정 특성을 보여주었다. 이중 $X=NO_2$ 화합물은 $S_A$상을 보였고, 나머지 화합물들은 모두 $S_B$상을 보여주었다. 화합물들의 녹음열은 일반적인 액정화합물들과 비교하여 낮은 값을 나타내었으며 등방화열은 비슷한 값을 보였는데, 치환기의 스멕틱그룹 효율성은 $H 순이었다.

• 약학회지
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• 제49권4호
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• pp.299-305
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• 2005

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 3,4-difluorophenyl (2a-5a), 4-hydroxyphenyl (2b-5b), 3-nitro­phenyl (2c-5c), 4-chlorobenzothiazoly (2d-5d) and 5-methylfurfural (2e-5e) instead of naphthyl group, and with hydrogen (3a-3e), methyl (4a-4e) and ethyl (5a-5e) in the place of methyl in naftifine were synthesized and tested for their in vitro anti-fungal activities against five different fungi. Fourteen compounds (3a, 4a, 5a, 3b, 4b, 5b, 3c, 4c, 5c, 3d, 4d, 3e, 4e and 5e) showed significant anti-fungal activities against T. mentagrophytes. (E)-N-(3-Phenyl-2-propenyl)-3,4-difluoro-ben­zenemethaneamine(3a), (E)_N_(3_phenyl_2_propenyl)_4_hydroxy_benzenemethaneamine(3b) and (E)-N-ethyl-N-(3-phenyl­2-propenyl)-3-nitro-benzenemethaneamine (5c) displayed moderate anti-fungal activities against all five different fungi.

• 한국환경독성학회:학술대회논문집
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• 한국환경독성학회 2003년도 춘계학술대회
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• pp.188-188
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• 2003

Examination was made of the urinary metabolite(s) of CKD-712, which is a chiral compound, named S-YS49 derived from higenamine (one component of Aconite spp.) derivatives. First of all, to analyze the metabolite(s) of CKD-712, a simple and sensitive detection method for CKD-712 was developed by using gas chromatography-mass spectrometry GC/MS). Urine was collected from adult male Sprague-Dawley rats 250${\pm}$10g) in metabolic cage for 24hr after oral administration of 100 mg/kg of CKD-712. The recovery of CKD-712 after extraction and concentration with AD-2 resin column was above 90 % from rat urine. The detection limits of CKD-712 in urine was approximately 0.1 ng/mL. It has well been suggested that isoquinoline possessing catechol moiety such as CKD-712 should be subjected to the catechol-O-methyl kransferase activity in vivo. We detected three major peaks of presumed CKD-712 metabolites in the total ion chromatogram obtained from the rat urine sample after oral administration of CKD-712. From these results, it is assumed that the urinary metabolites are mono-methylation in the naphthyl moiety (metabolite I ), methylation at the C-6 or 7 hydroxy group in the isoquinoline moiety and hydroxylation at in the naphthyl moiety (metaboliteII), and methylation at the C-6 or 7 hydroxy group in the isoquinoline moiety (metaboliteIII).

• Bulletin of the Korean Chemical Society
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• 제15권6호
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• pp.497-502
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• 1994

A new chiral stationary phase (CSP) for the liquid chromatographic resolution of enantiomers was prepared from (S)-naproxen and 3,5-dinitroaniline. The 6-alkoxy-2-naphthyl group of the CSP was presumed to act as a ${\pi}$-basic interaction site for resolving ${\pi}$-acidic racemates while the 3,5-dinitroanilide group of the CSP was presumed to play a role as a ${\pi}$-acidic interaction site for resolving ${\pi}$-basic racemates. From the chromatographic resolution trends of N-alkylamide derivatives of ${\alpha}$-arylalkylamines on the CSP prepared, the chiral recognition mode involving the intercalation of the amide alkyl chain of the less retained enantiomers between the connecting tethers of the CSP was proposed.

• Archives of Pharmacal Research
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• 제8권3호
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• pp.119-132
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• 1985

The apparent effectiveness of 1-naphthyl-N-methyl carbamate (carbaryl) against a wide variety of insects motivated the study of its mammalian toxicity. In this toxicological study of carbaryl, mature male rats inhaled carbaryl at a mean concentration of 112mg, 168mg and 224 mg/$m^{3}$ for one hour. After inhalation, pentobarbital sleeping time, Nadph-cytochrome c reductase activity, cytochrome p-450 and protein content in liver microsomes, various tissue residues, cholinesterase inhibition in plasma and histopathological findings at autopsy were observed. The pentobarbital sleeping time was prolonged in rats inhaled with carbaryl for one day while the sleeping time was shortened in the 3 days inhaled group. The changes of cytochrome p-450 content and NADPH-cytochrome c reductase activity exhibited biphasic response showing the decrease in the one day inhaled group and the increase in the 3 days inhaled group. The marked depression of plasma ChE activity was observed in rats inhaled with carbaryl at 112 mg/$m^{3}$, however no more progressive effect was observed at the higher concentration of the compound. The main observations in histopathological finding were ciliary detachment, epithelial swelling and subepithelial inflammatory cellular infiltration in trachea due to the irritation.

• Bulletin of the Korean Chemical Society
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• 제28권6호
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• pp.995-998
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• 2007

Pentacene moiety has been widely studied in Organic Thin-Film Transistor (OTFT) device as a channel layer because of high carrier mobility. In this study, we have fabricated vertical type Organic Static Induction Transistors (SITs) using pentacene, 6,13-Dinaphthalen-1-ly-Pentacene (1-DNP, 3), and 6,13-Dinaphthalen-2- ly-Pentacene (2-DNP, 4). 1-DNP and 2-DNP have same naphtyl group with pentacene, but different linked position and spatial arrangement. We have checked the static characteristics of materials in vertical type SITs device. We found that pentacene has as on/off ratio of 14.56, 1-DNP and 2-DNP shows as on/off ratio of 36.58 and 6.61 at VDS = 2V in SIT, respectively.