• Biomolecules & Therapeutics
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• 제31권1호
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• pp.108-115
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• 2023

Numerous psychotropic and addictive substances possess structural features similar to those of β-phenethylamine (β-PEA). In this study, we selected 29 β-PEA derivatives and determined their structure-activity relationship (SAR) to their ability to inhibit dopamine (DA) reuptake; conducted docking simulation for two selected compounds; and identified their potential functionals. The compounds were subdivided into arylethylamines, 2-(alkyl amino)-1-arylalkan-1-one derivatives and alkyl 2-phenyl-2-(piperidin-2-yl)acetate derivatives. An aromatic group, alkyl group, and alkylamine derivative were attached to the arylethylamine and 2-(alkyl amino)-1-arylalkan-1-one derivatives. The inhibitory effect of the compounds on dopamine reuptake increased in the order of the compounds substituted with phenyl, thiophenyl, and substituted phenyl groups in the aromatic position; compounds with longer alkyl groups and smaller ring-sized compounds at the alkylamine position showed stronger inhibitory activities. Docking simulation conducted for two compounds, 9 and 28, showed that the (S)-form of compound 9 was more stable than the (R)-form, with a good fit into the binding site covered by helices 1, 3, and 6 of human dopamine transporter (hDAT). In contrast, the (R, S)-configuration of compound 28 was more stable than that of other isomers and was firmly placed in the binding pocket of DAT bound to DA. DA-induced endocytosis of dopamine D₂ receptors was inhibited when they were co-expressed with DAT, which lowered extracellular DA levels, and uninhibited when they were pretreated with compound 9 or 28. In summary, this study revealed critical structural features responsible for the inhibition of DA reuptake and the functional role of DA reuptake inhibitors in regulating D₂ receptor function.

• 생명과학회지
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• 제16권2호
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• pp.323-327
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• 2006

아크릴아마이드의 형성과정에서 가열조건이 아크릴아마이드의 생성량과 아크릴아마이드 형성에 관여 또는 동반 생성하는 화합물을 조사하기 위하여, 아스파라긴과 포도당의 등량 혼합물을 125, 150, 175 및 $200^{\circ}C$에서 각각 10, 20 및 30 분간 가열하는 모델반응을 이용하였다. 가열한 반응물을 ethyl acetate 및 methanol 2종의 용매로 달리 추출하고 FFAP capillary column과 HP-5MS 5% phenyl methyl siloxane column으로 GC/MS에서 분석한 결과, 아크릴아마이드는 methanol추출물을 FFAP capillary column으로 분석한 결과에서 retention time 23.53분에서 검출되었고 최저검출한계는 4 ng 이었다. 아크릴아마이드 생성량은 $175^{\circ}C$보다. 낮은 125 및 $150^{\circ}C$에서는 온도와 가열시간을 증가시킬수록 점차 증가하여, $175^{\circ}C$에서 10분간 처리하였을 때 최대량인 $116{\mu}g/g$을 생성하였지만 175 및 $200^{\circ}C$에서는 온도 및 가열시간을 증가시킬수록 감소하는 결과를 나타내었다. 아크릴아마이드이외 반응생성물들로서, 1,3-dihydroxypropanone, 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyrane-4-one 및 5-hydroxymethylfurfural이 다량으로 검출되었으며, 또 다른 화합물인 5-methylfurfural, 2-acetylpyrrole 및 N,N-dimethylcyclohexamine 등은 소량 생성되었음을 확인하였다.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.258-269
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• 2002

2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

• Applied Biological Chemistry
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• 제28권3호
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• pp.196-201
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• 1985

Saccharomyces cerevisiae를 이용하여 합성배지중 질소원을 변화시키면서 생성된 향기성분을 조사한 결과 아미노산에 따라서 향기의 변화가 크게 나타났으며 특히 aspartic acid 배지는 전통적인 탁주향기, leucine배지는 휴젤유취 그리고 phenylalanine배지는 꽃향기등 흥미있는 향기를 발산하였다. 이들 배양액의 휘발성 화합물을 GC를 사용하여 분석한 결과 ethanol, iso-amyl alcohol, n-propanol이 주된 성분으로 밝혀졌으며 이외에 aspartic acid 배지에서는 phenethyl alcohol이 그리고 phenylalanine배지에서는 상당량의 phenethyl alcohol과 phenethyl acetate가 검출되었다.

• 공업화학
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• 제34권6호
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• pp.590-595
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• 2023

이미지 센서 컬러 필터에 사용하기 위해 새로운 황색 방향족 이민 유도체가 설계되고 합성되었다. 합성된 화합물은 방향족 이민 그룹을 기반으로 한 화학 구조를 가지고 있다. 새로운 재료는 상업용 장치 제조 공정을 모방한 조건에서 광학적 및 열적 특성을 기반으로 평가되었다. 이들의 관련 성능을 비교한 결과, ((E)-3-methyl-4-((3-methyl-5-oxo-1-phenyl-1H-pyrazol-4(5H)-ylidene) methyl)-1-phenyl-1H-pyrazol-5(4H)-one (MOPMPO)은 industry에 중점적으로 사용되는 프로필렌 글리콜 모노메틸 에테르 아세테이트 용매에 대한 용해도가 0.5 wt%이고, 290 ℃의 높은 분해 온도를 갖는 이미지 센서 컬러 필터 소재로서 우수한 성능을 나타내었다. MOPMPO가 이미지 센서 색재의 황색 염료 첨가제로 사용할 수 있음을 확인하였다.

• 대한전자공학회논문지
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• 제5권4호
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• pp.36-40
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• 1968

새로운 반사형 텔레비젼 디스푸레이를 소개한다. 이 방법에서는 선상의 액체결정의 다이나믹 스캣터링 모오드(Dynamic Scattering Mode, DSM)를 이용하며 주위가 밝은 곳에서도 볼 수 있다. 6∼12μm 두께의 액체결정은 뜯을 수 있는 음극선관 위에 와이어-모자의 훼이스 프레이트를 사용하는 전자속으로 실시간에 번지선택된다. 두가지 종류의 액체결정물질-Anasyliden Para-Amino Phenyl Acetate(APAPA)와 RCA 특유의 실온액체결정-을 시험했는데 동작온도(APAPA는 82°∼110℃이고 다른 것은 실온)를 제외하고는 비슷한 결과가 나왔다. 사방 3.1cm의 디스푸레이에서는 해상도가 적용 텔레비젼에 필요한 150line 보다 약간 떨여졌는데 그 원인은 액정결정 때문이 아니고 모자익의 구조에 의한 제한 때문이다. 더 나은 해상도를 얻으려면 디스푸레이를 좀더 크게하면 된다. 콘트라스트는 최적화(7.5:1)하지 않았다. 그러나 이 값을 정적인 디스푸레이에서 본 바와 같이 15∼20대 1로 개선하기 위해서는 몇가지의 기술을 사용할 수 있다. 이 디스푸레이 방법의 매력으로는 적당한 외부조명하에서는 약 ±45°의 넓은 관람각을 갖는데 있다고 하겠다. 액체결정내에서 DSM이 일어나도록 하는데 필요한 전류, 전압치들을 보면 평평한 텔레비젼 화면에 적합한 완전한 번지선택법에의 근사방법이 발견될 수 있으리라는 희망을 갖일 수 있다.

• Bulletin of the Korean Chemical Society
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• 제33권2호
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• pp.409-414
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• 2012

Xanthorrhizol is a bisabolane type of natural sesquiterpene, the major component of essential oils of Curcuma xanthorrhiza. 2-(3-Methoxy-4-methylphenyl)propan-1-ol and 2-(3-hydroxy-4-methyl phenyl)propan-1-ol could be essential building block for enantioselective synthesis of xanthorrhizol. Enantioselective (c = 53%, E = $80{\pm}3$) for R-(+)-2-(3-hydroxy-4-methylphenyl) propan-1-ol and (c = 58%, E = $27{\pm}1$) for R-(+)-2-(3-methoxy-4-methylphenyl) propan-1-ol resolution processes were developed via lipase-catalyzed reaction. We found lipase Aspergillus oryzae (AOL) and Porcine pancreas (PPL) are selective to transesterification and hydrolysis in organic and aqueous phase. Modified demethylated substrate is appropriate for enantioselective hydrolysis reaction without any additives. Enantiopure chiral alcohol was crystallized from ethyl acetate/n-hexane co-solvent system. Gram scale resolved chiral intermediate will facilitate the synthesis of the unnatural S-(+)-xanthorrhizol, the corresponding isomer of the natural one.

• 한국환경보건학회지
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• 제24권3호
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• pp.54-62
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• 1998

20 bacterial strains capable of growing on phenol minimal medium were isolated from soil and wastewater by the enrichment culture technique, and among them, one isolate which was the best in the cell growth was selected and identified as Bacillus sp. SH3 by its characteristics. Strain SH3 could grow with phenol as the sole carbon source up to 15 mM, but did not grow in minimal medium containing above 20 mM of phenol. The optimal conditions of temperature and initial pH for growth and phenol degradation were 30$^{\circ}$C and 7.5, respectively. This strain could grow on various aromatic compounds such as catechol, protocatechuic acid, gentisic acid, o-, m-, p-cresol, benzoic acid, p-hydroxybenzoic acid, anthranilic acid, phenyl acetate and pentachlorophenol, and the growth-limiting log P value of strain SH3 on organic solvents was 3.1. In batch culture, strain SH3 degraded 97% of 10 mM phenol in 48 hours. In continuous culture under the conditions of 20 mM of influent phenol concentration and 0.050 hr$^{-1}$ of dilution rate, the treatment rate of phenol was 94%.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.285.2-286
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• 2003

Analysis of illicit methamphetamine samples seized in Korea is discussed. The samples are extracted with the small portion of ethyl acetate under neutral conditions and the extracts are analyzed by GC-MS. Several impuritiy peaks are found in each chromatrogram. Eight compunds (1,2-Dimethyl-3-phenylaziridine, amphetamine oxime, ephedrine, N-formylmethamphetamine, N-acetylmethamphetamine, acetylephedrine, 3,4-dimethyl-5-phenyl-2-oxazolidone, methamphetamine dimer) are identified impurities in illicit methamphetamine and the identity of the impurity is conformed synthesis. (omitted)

• 약학회지
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• 제36권1호
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• pp.12-16
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• 1992

A new method for the synthesis of alminoprofen, which is a non-steroidal antiinflammatory agent, was described. Ethyl 2-phenyl-propionate(4) was prepared by Friedel-Crafts reaction of benzene with ethyl ${\alpha}-chloro-{\alpha}(methylthio)acetate(1)$, followed by methylation and desulfurization of the resultant ethyl 2-(methylthio)phenylacetate(2). Ethyl 2-(p-aminophenyl)propionate(6) was obtained by nitration of (4) and successive reduction of ethyl 2-(p-nitrophenyl)propionate(5). Alminoprofen was synthesized by reaction of (6) with methallyl chloride, followed by hydrolysis of the resultant ethyl 2-(p-methylallylaminophenyl)propionate (7).