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노인성 치매의 진단을 위한 비대칭 Biphenyl 중간체들의 합성
백승철,조천규 漢陽大學校 自然科學硏究所 1999 自然科學論文集 Vol.18 No.-
노인성 치매 (Alzheimer's disease) 는 대단히 파괴적이며 가장 널리 만연된 노인성 정신질환이다. 이 질병에 대한 적절한 치료법은 아직 개발되지 않은 상태이며 정확한 진단 또한 어려운 실정이다. 이 질병의 진단에는 환자의 뇌속에 침전된 아밀로이드라는 단백질 덩어리를 Congo Red를 사용해 염색하여 확인하는 방법이 가장 많이 사용된다. 감마선을 내는 ???Tc를 배위할 수 있도록 bipyridyl이 중앙에 위치한 몇몇 염료분자들을 합성하여 아밀로이드 침적물의 주성분인 β1-40 그리고 β1-42와의 흡착성을 조사해 본 결과 높은 binding affinity를 가짐이 확인되었다. 이 화합물들은 실제 뇌속에서 아밀로이드 침적물에 흡착되어 아밀로이드의 유. 무. 과. 다를 확인할 수 있겠으나 이들이 가진 charge와 큰 분자량 때문에 비선택적 BBB (Brain-blood barrier) opener가 필요할 것이라 예상된다. 이들의 BBB통과성을 높이기 위해 크기가 작으며 전기적으로 중성인 화합물 3을 디자인하게 되었다. 최종 화합물 3의 합성에 핵심 중간체로 사용되는 비대칭 biphenyl 화합물 9의 합성을 보고한다. Alzheimer's disease (AD) is highly destructive and most prevalent form of senile dementia, treatment of which is not currently available. It's diagnosis is based, in part, on the detection of neuritic amyloid plaques in the brains of demented patients by staining with the days Congo Red. Bipyridyl base dyes which can chelate radioactive γ-emitting ???Tc were shown to have high in vitro binding affinity for β1-40 and β1-42, principle constituents of the brain amyloid. They can be used as non-invasive chemical probes for the detection of amyloid deposits in brain with the aid of non-specific BBB openers. In order to increase BBB permeability, electrically neutral and much smaller ligand 3 was elaborated. We report synthesis of unsymmetric biphenyl moiety 9, the key intermediate for the final ligand 3.
Thermal cis-trans isomerization of triazo-benzene
최영욱,임영관,이상욱,조천규,이영일,손대원 한국물리학회 2007 Current Applied Physics Vol.7 No.5
1,3,5-Hydroxy-triazo-benzene (H-TAB) was synthesized through a coupling-oxidation protocol. Temperature-controlled UV, IR, andab initiocalculation were carried out to investigate the cistrans thermal isomerization of H-TAB. In temperature-controlled UV exper-iments,kmax of thepp* band and for the trans conformation at 335 nm and that for the cis form at 282 nm are shifted by increasedtemperature; band intensities of thepp* transition decrease andkmax of thepp* band is shifted toward the high-energy region. Themaximum peak at 2922 cm. 1 is shifted to 2926 cm. 1, and that at 2852 cm. 1 is shifted to 2856 cm. 1 at increased temperature in the tem-perature-controlled IR experiment.Ab initiobecause the cis form has less spatial repulsion. Therefore, the ground-state energy dierence induced by steric repulsion of the benzeneunit is the driving force of the blue shift in the thermal IR and UV spectra for the triazo-benzene.
Chiral Resolution of Racemic 2-Pyrone Diels-Alder Cycloadduct by Diastereomeric Salt Formation
전태홍,강형준,Anastasia Svirid,Alexander Lyakhov,Vitaly Kovalenko,조천규 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.9
An efficient protocol was developed that allows resolution of racemic bicyclolactone carboxylic acid obtained from the Diels-Alder cycloaddition of 3,5-dibromo-2-pyrone by formation of diastereomeric salts with quinidine and cinchonidine.
Synthesis of Functionalized Benzoxazoles and Their Binding Affinities to Aβ42 Fibrils
유경호,김동진,Young Shin Chun,Soo Jeong Lim,Seung Jun Oh,문대혁,조천규 대한화학회 2008 Bulletin of the Korean Chemical Society Vol.29 No.9
Functionalized benzoxazole derivatives were designed and synthesized based on the structural features of PIB and FDDNP, which show excellent binding affinities to aggregated Aβ 42 fibrils. All the synthesized compounds were evaluated by competitive binding assay against aggregated Aβ 42 fibrils using [125I]TZDM and displayed good in vitro binding affinities with Ki values (0.47-15.3 nM) from subnanomolar to nanomolar range. Among them, benzoxazoles 1f and 1a having malononitrile and ester moieties at C-6 exhibited superior binding affinities (Ki = 0.47 and 0.61 nM, respectively) to PIB (Ki = 0.77 nM).