• 대한화학회지
• /
• 제60권2호
• /
• pp.107-110
• /
• 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.

• Archives of Pharmacal Research
• /
• 제29권11호
• /
• pp.1006-1017
• /
• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• Bulletin of the Korean Chemical Society
• /
• 제21권6호
• /
• pp.562-566
• /
• 2000

$\beta-D-Mannopyranosyl$ disaccharides have been obtained from the coupling of 4,6-O-benzylidene derivatives of ethylthio $\alpha-D-mannopyranoside$ employing NIS-TfOH promoter. NIS-TfOH promoted couplings of the corresponding ethylthio $\beta-D-glucopyranoside$ and produced $\alpha-D-glucopyranosyl$ disaccharides. IDCP (iodonium dicollidine perchlorate) was inactive toward the 4,6-O-benzylidenated ethylthio glucopyranosyl donor. However,lDCP coupled the 4,6-O-benzylidenated $ethylthio-\beta-D-galactopyranoside$ to give a-D-galactopyranosyl disaccharides.

• 대한화학회지
• /
• 제42권1호
• /
• pp.78-83
• /
• 1998

Campylobacter jejuni 그램 음성균의 O-antigen 부위를 구성하는 삼탄당의 반복 단위를 합성하기 위해서 먼저 이들에 포함된 알트로헵토오스의 합성과 ${\alpha}$-알트로피라노시드를 선택적으로 형성시키는 방법을 개발하여야 한다. 본 연구에서는 알알 유도체에 선택적으로 1, 2-trans glycosidation을 시킴으로서 ${\alpha}$-알트로피라노시드 결합을 갖는 이당류를 합성하고자 하였다. 4, 6-O-Benzylidene-D-allal을 DMDO(3, 3-dimethyl diox-irane)와 반응시켜 1, 2-무수당 중간체를 만들고 아릴 알코올과 글루칼 유도체들과 반응시킨 결과 아릴 ${\alpha}$-알트로피라노시드 유도체와 ${\alpha}$-알트로피라노시드 결합을 갖는 이당류를 효과적으로 합성할 수 있었으며 마노오스등에서 간접적으로 ${\alpha}$-알트로피라노시드를 만드는 기존의 방법을 대체할 새로운 방법임을 확인 할 수 있었다.

• Bulletin of the Korean Chemical Society
• /
• 제19권11호
• /
• pp.1239-1244
• /
• 1998

Derivatives of ethylthio α-D-mannopyranoside as glycosyl donors are compared in coupling efficiency and stercoselectivity with varying thiophilic promoters from methyl triflate (MeOTf), dimethyl(methylthio)sulfonium triflate (DMTST) to iodonium dicollidine perchlorate (IDCP), solvents and glycosyl acceptors. IDCP was the most efficient promoter in coupling of perbenzylated ethylthio-α-D-mannopyranosides (1 and 2), giving α-Dmannosyl disaccharides preferentially, whereas inactive in coupling of 4,6-O-benzylidene derivatives 3 and 4. MeOTf and DMTST promoted coupling of 4,6-O-benzylidene derivatives 3 and 4, but P-D-mannopyranosyl disaccharides were formed preferentially. Coupling reaction was retarded as solvent polarity decreased.

• 약학회지
• /
• 제6권1호
• /
• pp.17-18
• /
• 1962

Several polygalitol derivatives, 4,6-benzylindene-polygalitol, 2,3-diacetyl-4,6-benzylidene-polygalitol and 2,4-diacetyl-polygalitol which might be useful to the preparation of partial condensation products of polygalitol, have been described.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
• /
• pp.252.3-252.3
• /
• 2003

An effective and convenient regioselective reduction of 5-benzylidene 2,4-thiazolidinedione derivatives to the corresponding 5-benzyl 2,4-thiazolidinedione derivatives has been accomplished using 3,5-dicarboethoxy-2,6-dimethyl-1,4-dihydropyridine (Hantzsch dihydropyridine ester: HEH) with silica gel as an acid catalyst in a good yield.

• 한국산학기술학회논문지
• /
• 제4권3호
• /
• pp.260-262
• /
• 2003

A thermal vapor deposition method for crystallization of insoluble analytes with matrix is established as a new sample preparation method for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS). A mixture of mono, bis and tris(p-ethyl benzylidene) sorbitols was incorporated into microcrystals of ferulic acid, which was confirmed by confocal micrographs. Molecular masses of sorbitol derivatives were determined in this way by MALDI-MS without thermal decomposition.

• 한국산학기술학회:학술대회논문집
• /
• 한국산학기술학회 2003년도 춘계학술발표논문집
• /
• pp.311-313
• /
• 2003

A thermal vapor deposition method for crystallization of insoluble analysis with matrix is established as a new sample preparation method for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS). A mixture of mono, bis and tris(p-ethyl benzylidene) sorbitols was incorporated into microcrystals of ferulic acid, which was confirmed by confocal micrographs. Molecular masses of sorbitol derivatives were determined in this way by MALDI-MS without thermal decomposition.

• Bulletin of the Korean Chemical Society
• /
• 제22권5호
• /
• pp.476-480
• /
• 2001

4-Thiazolidinones which are hetarylsubstituted at the 2-position were prepared by the reaction of mercapto acids with aldimines which were prepared by the condensation of pyrrole-2-carbaldehyde with different aromatic amines. After their benzylide ne derivatives were obtained, we first applied the Wittig reagent on them in the presence of triethylamine, dihydrofurothiazolidines were synthesized. Second, we prepared new pyrazolinothiazolidines by using phenylhydrazine in the presence of sodium acetate. All mentioned compounds have been characterized by their spectral data, and screened for their antimicrobial activities. Some of them exhibit moderate to good antibacterial and tuberculostatic activities.