• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
• /
• pp.189.1-189.1
• /
• 2003

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5-aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A$_3$ receptors. A methoxy group in the 4-position of the phenyl ring and N-acetyl or propionyl substitutions of the aminothiazole and aminothiadiazole templates displayed great increases of binding affinity and selectivity for human adenosine A$_3$ receptors. The most potent A$_3$ antagonist of the present series, N-［3-(4-methoxy-phenyl)-［1,2,4］thiadiazol-5-yl］-acetamide exhibiting a K$\_$i/ value of 0.79 nM at human adenosine A$_3$ receptors, showed antagonistic property in functional assay of cAMP biosynthesis involved in one of the signal transduction pathways of adenosine A$_3$ receptors. (omitted)

• 대한화학회지
• /
• 제58권1호
• /
• pp.62-67
• /
• 2014

In the present study a novel series of (2-substituted-4-methylthiazol-5-yl)(4-substituted piperazin-1-yl)methanone derivatives were synthesized by reaction of 2-substituted-4-methylthiazole-5-carboxylic acid with N-substituted benzyl piperazine by using 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide hydrochloride (EDCl) and 1-hydroxybenzotriazole (HOBt) in DMF. All the newly synthesized compounds were characterized by spectral methods. The title compounds were screened for in vitro antibacterial activity. Most of the compounds show moderate to good antimicrobial activity.

• Archives of Pharmacal Research
• /
• 제29권1호
• /
• pp.16-25
• /
• 2006

A novel series of 1-(1-benzofuran-2-yl-ethylidene)-4-substituted thiosemicarbazides (2a-d) along with some derived ring systems: substituted-2,3-dihydro-thiazoles(3a-c, 4a-f) and thiazolidin-4-ones(5a-d and 6a-d), were synthesized. In addition, cyanoacetic acid-(1-benzofuran-2-yl-ethylidene) hydrazide(7) was used to prepare another new series of compounds consisting of substituted pyridin-2(1H)-ones(8a-c); 2-thioxo-2,3-dihydro-thiazoles(9a-d) and 2-thioxo-2,3-dihydro-6H-thiazolo[4,5-d]pyrimidin-7-ones (10a-c, 11a-c). The absolute configuration of compound 5c was determined by X-ray crystallography. The compounds prepared were evaluated for their in vitro anti-HIV, anticancer, antibacterial, and antifungal activities. Among the tested compounds, compounds 5c and 9a produced a significant reduction ㅐ ㄹ the viral cytopathic effect (93.19% and 59.55%) at concentrations $>2.0{\times}10^{-4}\;M\;and\;2.5{\times}10^{-5}\;M$respectively. Compound 9a was confirmed to have moderate anti-HIV activity. Compounds 2a, 2d, and 5c showed mild antifungal activity. However, none of the tested compounds showed any significant anticancer activity.

• 한국식품영양과학회지
• /
• 제41권1호
• /
• pp.116-122
• /
• 2012

흑마늘은 일정기간 마늘의 자체 성분과 효소 등에 의해 숙성되어 진한 흑갈색으로 변한 것으로 추출액과 같은 가공형태로 시중에 많이 유통되고 있으나 관능적 품질평가에 대한 연구는 아직 미흡한 실정이다. 본 연구에서는 국내 흑마늘 제품의 산지별에 따른 흑마늘추출액 4종(A, B, C, D)을 선정하여 관능적 요소 중 가장 중요한 휘발성 향기성분을 분석하여 제품의 품질에 대한 기초자료로 활용하고자 하였다. 시판 흑마늘추출액의 휘발성 향기성분을 분석한 결과, 총 68종으로 함황화합물류 21종, 알데히드류 10종, 퓨란류 7종, 알콜류 6종, 방향족화합물 7종, 케톤류 4종, 산류 4종, 질소화합물 3종, 에스테르류 2종 및 기타 4종이 검출되었다. 흑마늘추출액 모든 시료에서 fruit-sweet향의 2,6-dimethyl-4-heptanone이 높은 함량 검출되었다. 함황화합물에서는 6종, allyl sulfide, 4-methyl-1,2,4-thiazole, 1,3,5-trithiane, unknown I(RI 1564), II(RI 1565), III(R I1613)이 전 시료에서 높은 함량 검출되었으며, 마늘향기성분에 관여할 것으로 사료된다. 또한 Maillard 반응에 의해 형성되어지는 것으로 알려진 3종의 알데히드류(3-methylbutanal, benzaldehyde, phenylacetaldehyde)와 4종의 furan류(furfural, 2-acetylfuran, 5-methyl-2-furfural, furfuryl alcohol), 2,6-dimethyl pyrazine, acetic acid가 모든 시료에서 높은 함량으로 검출되었으며, 이들 향기성분들은 시판 흑마늘추출액의 휘발성성분에 burnt, sweet, sour한 특징적인 냄새에 기여할 것으로 사료되었다.

• 생명과학회지
• /
• 제13권1호
• /
• pp.54-58
• /
• 2003

새로운 농약을 창출하기 위해, thiazole 유도체 등에서 살균력이 존재하는 구조를 가진 1,2-benzisothiazole-3-one-1,1-dioxide를 선도물질로 imidazolidinetrionyl 기를 가진 새로운 화합물을 합성하였다. 1-methylurea와 oxalyl chloride의 반응으로부터 4단계 반응을 거쳐 1-methyl-3-(1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl) -imidazolidine-2,4,5-triones 5a, 1-ethyl-3- (1,1,3-trioxo-1,3-dihydro-1λ$^6$-benzo[d] isothiazo1-2-ylmethyl)-imidazolidine-2,4,5-triones 5b, 1-phenyl-3-(1,1,3- trioxo-1,3-dihydro-1λ$^6$-benzo[d]isothiazol-2-ylmethyl)-imidazolidine-2,4,5-triones 5c를 합성하였다. 합성된 5a, 5b, 5c를 식물반응, 곤충 그리고 살균제 등에 대한 생물학적 반응검색을 하였다. 생물학적 반응검색 결과(식물반응 검색은 5b, 곤충검색은 5a, 그리고 살균제 검색은 5a에서 생물활성이 조금 나타남) 썩 좋은 반응결과를 얻지 못했다. 하지만 계속해서 2,4,5-imidazolidinetrionyl기를 가진 saccharin유도체를 합성하여 새로운 농약을 창출하고자 한다.

• Journal of Microbiology and Biotechnology
• /
• 제13권1호
• /
• pp.43-49
• /
• 2003

Metabolism of a new fungicide ethaboxam by soil fungi was studied. Among the fungi tested, Cunninghamelia elegans produced metabolites from ethaboxam, which were not found in the control experiments. M5, a major metabolite from ethaboxam was firmly identified as N-deethylated ethaboxam by LC/MS/MS and NMR. N-Deethylated ethaboxam has been found as a single metabolite in in vitro metabolism with rat liver microsomes. Ml was proved to be 4-ethyl-2-(ethylamino)-1,3-thiazole-5-carboxamide (ETC) by comparing with the authentic compound. In addition, M2, M3, and M4, and M6 were tentatively Identified by LC/MS/MS as hydroxylated and methoxylated ethaboxams, respectively. Production of the major metabolite, N-deethylated ethaboxam, by the fungus suggested that C. elegans would be an efficient eukaryotic microbial candidate for evaluating xenobiotic-driven mammalian risk assessment.

• 대한임상검사과학회지
• /
• 제39권1호
• /
• pp.19-24
• /
• 2007

The aim of this study was to evaluate the bacterial effects of Moraxella catarrhalis in otitis media with effusion (OME) by photodynamic therapy (PDT). Bacterial suspensions (10000 CFU/mL) were prepared. The colony forming units (CFU) of Moraxella catarrhalis have been measured after an application of photogem plus 632 nm diode laser irradiation. One ml of the bacterial suspensions have been incubated in the dark for 3h with various concentrations of photogem ($0.625{\sim}5.0_{\mu}g/mL$) and then irradiated with 632 nm diode laser ($15J/cm^2$). After, the PDT Moraxella catarrhalis suspensions ($50{\mu}L$) were inoculated on chocolate agar plate and cultured in the dark at $37^{\circ}C$, 5% $CO_2$ condition for 18h. The colony forming units off the bacteria were measured. Also transmission electron microscopy (TEM) was employed to evaluate the effect of otitis media pathogens by PDT. The nucleus of Moraxella catarrhalis was stained using green fluorescent nucleic acid dye thiazole orange and the fluorescence intensity of the nucleus was measured by flow cytometry. The PDT was effective in killing Moraxella catarrhalis at the photogem dose of $5.0_{\mu}g/mL$, respectively, As assessed by flow cytometry analysis the fluorescence intensity of the nucleus got lower after PDT. TEM result appeared to able to cause damage to the bacterial membranes. On the basis of these findings, bacterial photodynamic therapy with photogem can be considered to be a promising new therapeutic approach for OME.

• 한국식품과학회지
• /
• 제26권6호
• /
• pp.781-786
• /
• 1994

HVP를 기본 원료로 하여 몇몇 반응 전구물질을 첨가하여 여러 가지 반응 조건에 따라 meatlike flavor를 제조하였다. pH와 온도는 반응액의 갈변화도에 큰 영향을 미쳐, pH와 온도가 높을수륵 갈변화 속도는 빨라졌다. 반응액에 잔존하는 환원당과 유리 아미노산은 반응 1시간까지 급격히 감소하였으나 반응 온도의 영향은 거의 받지 않았다. 각 아미노산의 경우, glutamic acid와cysteine은 반응 시간이 경과함에 따라 감소하나, glycine과 methionine은 거의 변화가 없었다. Maillard 반응을 통해 생성되는 meatlike flavor외 향기 성분은 49종이 통정되었으며, 이중에 3-methyl butanal, 2-methyl tetrahydrothiophen-3-one, 3,4-d imethyl thiophene, 2,4-dimethyl thiagole 둥의 잘 알려진 natural meat flavor 성분들도 포함되어 있었다. $120^{\circ}C$에서 제조된 반응액을 관능 평가한 결과, 반응 1시간대의 반웅액이 5% 유의수준에서 구수한 맛이 가장 강하였고, 이미가 가장 적었다. 이상의 결과에서, 본 반응 system에서는 반웅 1 시간내에 대부분의 Maillard 초기 반응이 일어나고, 그이후, 반응이 진행될수록 구수한 맛을 내는 성분은 줄어들고, 이미를 나타내는 성분이 증가한다고 추정되었다.