• 대한화학회지
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• 제21권2호
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• pp.139-148
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• 1977

2-푸르푸랄과 5-알킬-2-푸르푸랄류 가운데 5-메틸-2-푸르푸랄, 5-이소프로필-2-푸르푸랄, 5-삼차부틸-2-푸르푸랄, 5-이소아밀-2-푸르푸랄, 그리고 5-니트로-2-푸르푸랄 등의 옥심 생성반응 속도 정수를 pH 7인 완충용액내 반응온도 15∼$45^{\circ}C$에서 구하였다. 이 반응은 2차반응이며 활성화 에너지는 각각 5.50, 7.22, 7.03, 7.49, 7.78 그리고 4.97 kcal/mole이다. 5-알킬-2-푸르푸랄류에 대하여는 Hammett식이 성립되고 반응온도 15, 25, 35, $45^{\circ}C$에서 반응정수는 각각 2.010, 1.756, 1.541, 1.311 등이 계산되었다.

• 한국지역사회생활과학회지
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• 제16권2호
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• pp.3-9
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• 2005

The study was carried out to evaluate the antimutagenic and anticancer effects of small water dropwort. The methanol extracts from small water dropwort significantly reduced the mutagenicity induced by aflatoxin $B_1\;(AFB_1)$ and N-methyl-N'-nitro-N-nitrosoguanidine(MNNG) in Salmonella typhimutium TA 100. Also, the methanol extracts inhibited the growth of AZ-521 human gastric cancer cells and HT-29 colon cancer cells. The chloroform fraction from methanol extracts of small water dropwort inhibited $40\;to\;80\%$ of the mutagenicity by $AFB_1$ in Sal. typhimurium TA 100 by the addition of 2.5 to $10\%$. To separate active compounds, the chloroform fraction was subjected to column chromatography on a silica gel and separated into five fractions. Among the five fractions, fraction 4 showed the highest antimutagenic effect against $AFB_1$ and an anticancer effect in the HT-29 colon cancer cell. As the result of the analysis in GC-MS, 1-napthalene carbonitrile, 5,6,7,8-tetrahydrol and benzene, 1,1'-(1,4-pentadiene-1,5-diyl) bis-,(E,E) were identified potentially from fraction 4.

• Archives of Pharmacal Research
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• 제19권2호
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• pp.163-167
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• 1996

Aloe plants have been used as herbal medicine for centuries and the name aloe means the dried exudate from the cut leaves of Aloe ferox Mill. (Cape aloe, Liliaceae), Aloe ferryi Baker. (Socotrine aloe), A. bainesii Th. Dyer. (Natal aloe) and Aloe vera L. (Curacao aloe) (Namba, 1986). Among them, Aloe vera has not only been one of the most used natural drug well known for its cathartic properties, but also has been widely used as raw materials of cosmetics and health foods (Leung, 1978, Hoffenberg, 1979). Although previous investigations showed that the leaves of A. vera contain a number of anthracene and chromone derivatives such as aloin A, aloin B, 1, 3, 6, 8-tetra-nitro-4,5-dihydroxy-2-hydroxymethyl anthraquinone and 7-hydroxy-aloin, its chemical composition is far from being completely investigated (Hoffenberg, 1979, Rauwald and Voetig, 1982). As a part of our chemical investigations on the constituents of aloe, we report chemical investigation of the freeze dried ground leaves of A. vera which is led to the isolation of five compounds from the ethyl acetate soluble fraction of the methanolic extract.

• Biomolecules & Therapeutics
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• 제2권2호
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• pp.155-160
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• 1994

Human immunodeficiency virus type 1 (HIV-1) protease is essential for the replication of the virus and it is therefore an attractive target for antiviral drugs of HIV-1. Several dipeptide isosteres containing 2-isoxazoline or $\alpha$-hydroxy ketomethylene have been synthesized and their inhibitory effects on the HIV-1 protease examined. The enzymatically active HIV-1 protease was purified to homogeniety from E. coli transformed with a recombinant plasmid (pMAL-pro) containing the entire gene encoding the protease. The purified protease had the substrate specificity with Km value of 9.8$\mu$M when an undecapeptide His-Lys-Ala-Arg-Val-Leu-(p-nitro)Phe-Glu-Ala-Nle-Ser-amide was used as a substrate, and the products from the substrate after specific cleavage by HIV-1 protease were analyzed by HPLC. The synthetic compounds containing dipeptide isosteres showed specific inhibitory effects while a dipeptide isostere containing an isoxazoline ring inhibited the HIV-1 protease competitively with Ki value of 500 $\mu$M. Even if the inhibition effects of HIV-1 protease were not very high, these novel dipeptide isosteres can be used as key structural moieties for developing specific inhibitors of HIV-1 protease.

• 한국추진공학회지
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• 제23권5호
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• pp.53-59
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• 2019

고체연료는 추진제 연소 시 산화제와 반응하여 추진제 성능을 증가시키는 역할을 한다. 대표적인 고체연료는 Al, RDX, HMX 등이 있다. 이들 물질은 연소 시 수분과 만나 흰색 연기를 발생시키고, 일산화탄소, 이산화탄소, 메탄가스 등의 환경유해 물질을 다량 발생시킨다. 이러한 문제를 해결하기 위해 본 연구에서는 고체 연료로 사용 가능한 고질소 에너지 물질인 hydrazinium 5-aminotetrazolate(HAT)를 제조하였다. 분광분석(NMR)을 통해 HAT의 구조를 분석하였으며, DSC를 이용하여 열특성 분석을 하였다. 또한, EXPLO5 프로그램을 이용하여 비추력, 가스발생량 등을 계산하였다.

• 분석과학
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• 제36권4호
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• pp.143-151
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• 2023

Considering the greater role of α-amino acids in our daily lives, the enantiomer resolution of seven α-amino acids derivatized with fluorogenic reagent (4-fluoro-7-nitro-2,1,3-benzoxadiazole, NBD-F) by chiral HPLC on amylose or cellulose trisphenylcarbamate derived chiral stationary phases (CSPs) under simultaneous ultraviolet (UV) and fluorescence (FL) detection was performed. The degree of enantioseparation and resolution was affected by nature and selector backbones of the CSPs as well as the kind of amino acids. Baseline enantiomer separation and resolutions were observed for the enantiomers of all analytes as NBD derivatives especially on coated type amylose tris(3,5-dimethylphenylcarbamate) derived CSPs (Chiralpak AD-H and Lux Amylose-1). The other CSPs also showed good enantioselectivity except for the CSPs (Chiralpak IB, Chiralcel OD-H and Lux Cellulose-1) having cellulose tris(3,5-dimethylphenylcarbamate) as chiral selectors. The developed analytical chiral method was applied to determine the enantiomeric purity of seven commercially available L-α-amino acids and the impurities as D-forms were found to be in the range 0.08-0.87 %, respectively. The intra- and interday accuracy and precision assays showed high accuracy and precision of the developed analytical method. This chiral HPLC method for the enantiomer resolution of amino acids using fluorescent derivatization could be useful for the determination of enantiomeric purity of pharmaceuticals and biological study for amino acid type compounds among chiral drugs.

• Nuclear Engineering and Technology
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• 제5권1호
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• pp.44-54
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• 1973

방사성 $^{38}$ CL로 표지된 유기 하로겐 화합물의 제조방법을 가려내기 위하여서 Phenyl halides(7종), thloro nitrobenzene(6종), Chloro nitroanisole(2종), Chloro aniline (3종), Chloro anisidine(3종), Chloro toluene(3종), Benzyl chloride 유도체(4종) 및 기타 대조 화합물 3종 등을 원자로 내에서 조사하고 생성물을 알카리 수용액으로 주출하고 각각의 무기 $^{38}$ CL 수율을 조사시간 별로 검토하였다. 그 결과 화합물의 구조 보다도 표적물의 상태에 따라서 무기물 수율에 변화가 있고 고체상의 표적물의 경우에는 수율이 일반적으로 얕고 변화가 고르다는 것을 화인 하였다. 화학구조에 따르는 무기 $^{38}$ CL0의 생성수율의 감소는 현재까지의 결과로 보아서 Phenyl chlorides$^{38}$ CL 수율간에 Linear relationship가 있었으며 염소원자수가 많을수록 그 수율이 얕았다. 실험 결과를 논의하였으며 교지 반응에 대한 본 실험 결과의 응용성가능 여부를 고찰하였다.

• Applied Biological Chemistry
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• 제39권2호
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• pp.140-146
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• 1996

Imidacloprid와 일련의 새로운 1-(6-chloro-3-pyridylmethy)-3-N-nitroimidazolidin-2-ylideneamine 유도체들을 합성하고 imidazolidine고리의 3-N-치환기(R) 변화에 따른 구조와 벼멸구(Nilaparvata lugens) 및 복숭아 혹 진딧물(Myzus persicae)에 대한 선택적인 살충활성 관계(SAR)를 검토한 바, 벼멸구에는 STERIMOL 파라미터인 B1상수$({\AA})$보다 소수성$({\pi})$, 그리고 복숭아 혹 진딧물에는 입체상수(Es)보다 극성 치환기상수$({\sigma}^{ast})$ 큰 변수로 작용하였다. 벼멸구의 경우에는 ${\pi}$상수의 적정값이 0.52이고 복숭아 혹 진딧물의 경우에는 $\sigma^{\ast}$상수의 적정값이 1.17로 이들 값에 가까운 값을 갖는 치환체일수록 큰 살충활성이 예상되었다. 두 경우, 모두 공통적으로 methyl 및 benzenesulfonyl-치환체(7 및 8)와 같은 센 전자끌게들은 살충활성에 기여하지 않았다. 그러나, 비치환(H)체(1)인 imidacloprid는 가장 큰 살충활성을 나타내었으며 H의 ${\pi}$상수와 ${\sigma}^{\ast}$상수가 이들 두 상수의 적정값에 미치지 못하지만, 양호한 살충활성을 나타낸 까닭은 2-N-nitro group의 산소원자와 3-imid group의 수소원자 사이에 형성된 분자내 회합(H-결합)에 기인함을 알았다. 그리고 pH 6.0 이하의 산성 수용액에서는 대단히 큰 잔류성을 나타내었으며 $45^{\circ}C$의 pH 7.0에서$(K_{obs};5{\times}10^8sec.^{-1})$ 반감기(t1/2)는 대략 6개월이었다.

• 대한화학회지
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• 제5권1호
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• pp.33-37
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• 1961

We have shown that carboxy-peptidase destroys the biological activity of angiotensin octa-and deca-peptides. Since Proline occurs as the seventh amino acid from the amino end of the chain and since carboxypeptidase does not cleave proline from a peptid chain, it is evident that the heptapeptid H.asp-arg-val-tyr-ileu-his-pro.OH is formed by this hydrolysis. This peptide must then be biologically inactive. In order to determine whether the phenyl group of the C-terminal amino acid was the necessary requirement for biological activity of the octapeptide, $ala^8$ angiotensin octapeptide(amino acids of peptides numbered from amino end) was synthesized. For this synthesis the four dipeptides were prepared: carbobenzoxy-L-prolyl-L-alanine-P-nitrobenzyl-ester, m.p. $134-135^{\circ}C,$ carbobenzoxy-L-isoleucyl-imidazole benzyl-L-histidine methyl ester, m.p. $114-116^{\circ}C,$ carbobenzoxy-L-valyl-L-tyrosine hydrazide and carbobenzoxy B-benzyl-L-aspartyl-nitro-L-arginine. The first three dipeptides were obtained as crystalline compounds. Imidazole-benzyl-L-histidine was used in the hope that it would block the histidine imidazole against side reactions in steps subsequent to the formation of the C-terminal tetrapeptide. Also, it was through that the imidazole benzylated peptides would be easier to crystallize. This, however, was not the case. The tetrapeptide, carbobenzoxy-L-isoleucyl-L-im, benzyl-histidyl, L-prolyl-L-alanine-nitrobenzyl ester was not obtained in a crystalline form. Neither could the mono-or dihydrobromide of the tetrapeptide free base be induced to crystallize. Carbobenzoxy-L-valyl-L-tyrosine azide was condensed with the tetrapeptide free base to yield the protected hexapeptide; carbobenzoxy-L-valyl-L-tyrosyl-L-isoleucyl-L-im, benzyl, histidyl-L-Prolyl-L-alanine-nitrobenzyl ester. Upon removal of the carbobenzoxy group with hydrogen bromide in acetic acid an amorphous free base hexapeptide ester was obtained. This compound gave the correct C, H, N analysis and contained the six amino acids in the correct ratio. The octapeptide was obtained by condensing this hexapeptide with carbobenzoxy-B-benzyl-L-aspartyl-nitro, L-arginine using the mixed anhydride method of condensation. This amorphous product was proven to be homogenous by chromatography in two solvent systems and upon hydrolysis yielded the eight amino acids in correct ratio. The five protecting groups were removed from the octapeptide by hydrogenolysis over palladium black catalyst. Biological assay of the free peptide indicated that it possessed less than 0.1 per cent of both pressor and oxytocic activity of the phenylalanine8 angiotensin. This suggests that the phenyl group is a point of attachment between angiotensin and its biological receptor site.

• 대한화학회지
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• 제48권1호
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• pp.28-32
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• 2004

초임계 이산화탄소 용매에서의 (벤질렌)삼페닐 인 일리드 화합물의 카르보닐 화합물과의 Wittig 반응을 연구하였다. 소량의 조용매 (THF, 5%)를 첨가한 이산화탄소 (24 mL 용기)에 녹인 (벤질렌)삼페닐 인 일리드 (약 1 mmol)를 여러 방향족 알데히드와 초임계 조건(80 $^{\circ}C$, 2,000 psi) 에서 2시간 반응시켜 올레핀 화합물을 좋은 수율로 얻을 수 있었다. 새로운 조건에서의 반응은 기존 용매 (THF)에서의 반응보다는 약간 느리게 나타났으나 생성물의 (E)- 와 (Z)-이성체 비율에 차이가 있었다. 두 이성체가 함께 생성되는 반응의 경우 (Z)-이성체의 비율이 증가하였다. 반면 t-butylcyclohexanone과 같은 케톤과의 반응은 두 조건에서 모두 낮은 전환을 보였다. 이 연구를 통하여 이산화탄소에서의 Wittig 반응이 초임계 조건에서 좋은 수율로 이루어지며 이 새로운 용매의 사용으로 반응선택성의 변화가 가능할 수 있다는 초기 결과를 얻었다. 이 결과는 Wittig 반응과 같은 유용한 유기반응을 친환경 용매 (이산화탄소)에서 수행할 수 있도록 전환하는데 좋은 자료가 될 수 있다고 본다.