• 대한화학회지
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• 제42권1호
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• pp.1-8
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• 1998

티아졸 고리를 포함하는 lexitroposin에서, DNA minor groove의 염기쌍과 결합하는 부분인 티아졸의 분자정전기전위를 ab initio계산을 통해 구하였으며 protonate된 티아졸의 두 가지 가능한 형태에 대해 MNDO 및 ab initio방법으로 기하학적 구조를 최적화 하였다. 최적화된 구조에 대해 6-31G및 6-31G* basis set을 사용하여 양성자 친화도를 구하였으며 아울러 티아졸의 양성자 친화도에 미치는 치환기 효과를 알아보기 위해 전자를 주는 기와 전자를 끄는 기를 치환시킨 여러 치환 치아졸에 대해 양성자 친화도를 조사하였다. 그 결과 티아졸의 질소 원자가 DNA minor groove 쪽으로 배향되고 전자를 주는 기가 치환될 때 양성자 친화도가 증가됨을 알 수 있었다.

• Archives of Pharmacal Research
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• 제27권11호
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• pp.1081-1085
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• 2004

Several 2-[[(benzoxazole/benzimidazole-2-yl)sulfanyl]acetylamino]thiazoles derivatives were synthesized by reacting 4-substituted-2-(chloroacetylamino)thiazoles with benzoxazole/benzimidazole-2-thioles in acetone and in the presence of $K_2CO_3$. The chemical structures of the compounds were elucidated by IR, $^1H-NMR$, and $FAB^{+}-MS$ spectral data. Their antimicrobial activities against Micrococcus luteus (NRLL B-4375), Bacillus cereus (NRRL B-3711), Proteus vulgaris (NRRL B-123), Salmonella typhimurium (NRRL B-4420), Staphylococcus aureus (NRRL B-767), Escherichia coli (NRRL B-3704), Candida albicans and Candida globrata (isolates obtained from Osmangazi Uni. Fac.of Medicine) were investigated and in this investigation, a significant level of activity was illustrated.

• 대한화학회지
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• 제55권5호
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• pp.882-886
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• 2011

• Bulletin of the Korean Chemical Society
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• 제33권12호
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• pp.4271-4274
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• 2012

• 공업화학
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• 제20권2호
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• pp.134-139
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• 2009

(E)-3-(Aryl)acrylaldehyde 유도체들 (1a~1e)과 thiosemicarbazide 축합반응으로 일련의 알릴리덴치오세미카르바존 화합물 (2a~2e)을 45~85%로 얻었다. 이 화합물들을 2,4'-dibromoacetophenone와 2,3-dichloroquinoxaline로 처리하여 각각 2,4-이치환 티아졸류(3a~3e)와 2-[(E)-3-(aryl)allylidenehydrazone]thiazolo[5,4-b]quinoxaline류 (4a~4e)를 좋은 수율로 합성하였다. 새로이 합성한 모든 화합물들의 구조들은 IR과 $^1H-NMR$ 분광학 자료로 확인하였다.

• 대한화학회지
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• 제60권2호
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• pp.107-110
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• 2016

A new series of hydrazino thiazolyl-2-azetidinone 4(a-i) derivatives were synthesized efficiently using benzylidene hydrazinyl thiazole derivatives 3(a-i). The precursors, benzylidene hydrazinyl thiazoles were prepared by reacting 4-fluoro phenacyl bromide with thiosemicarbazones 2(a-i). All the structures of the synthesized compounds were ascertained by IR, NMR and mass spectral analysis.

• 약학회지
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• 제29권1호
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• pp.39-42
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• 1985

Betaines of bicyclic imidazo-thiazoles were synthesized by the reaction of clectrophiles such as methyl isocyanate, methyl isothiocyanate, allyl isothiocyanate and ketene with 3-methyl and 3-phenyl-5, 6-dihydroimidazo [2,1-b] thiazole. In this reaction, the methyl group which was substituted at 3-position increased the yields of the products in comparison with those from phenyl group substituted substrates. Also, the betaines reacted with methyl iodide to give imidazo-thiazolium salts which were unstable at high temperature and converted the quaternary ammonium salts of original biheterocycles.

• Bulletin of the Korean Chemical Society
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• 제34권1호
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• pp.271-274
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• 2013

• Archives of Pharmacal Research
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• 제16권4호
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• pp.318-321
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• 1993

Cyanoaccetic acid hydrazide reacted with some 2-pyrazolin-5-one, isoxazol-5-one and 2-thiazolin-4-one and their ylidene derivatives to yield several new annelated pyran heterocycles. Structures wre established on the basis of elementary analyses and spectral data studies in addition to synthesis via other routes.

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