• YAKHAK HOEJI
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• v.41 no.2
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• pp.174-180
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• 1997

Four oxazolidinone analogues(6, 7, 8, 9), which are isosters of 5, were synthesized by the reaction of 2-chloroalkyl-3,5-dimethyl-4-methoxypyridine with the corresponding benzox azolidinone or oxazolidinone, respectively, and were evaluated for their inhibitory activities toward proton pump enzyme under in vitro condition. Isosteric substitution of the benzothiazolidine moiety in 5 with benzoxazolidinone rendered the molecule relatively inactive.

• Bulletin of the Korean Chemical Society
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• v.31 no.11
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• pp.3341-3347
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• 2010

A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by $^1H$-NMR, $^{13}C$-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of $1\;g\;L^{-1}$.

• Archives of Pharmacal Research
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• v.22 no.6
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• pp.624-628
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• 1999

A formal asymmetric synthesis of Mugineic acid was accomplished from cis-2-butene-1,4-diol throughcatalytic Sharpless epoxidation oxidations and doupling reaction.

• Bulletin of the Korean Chemical Society
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• v.34 no.2
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• pp.641-644
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• 2013

• YAKHAK HOEJI
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• v.57 no.2
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• pp.95-100
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• 2013

This study was performed to analyze in vitro and in vivo activities of LCB01-0183, a new oxazolidinone, against clinical isolates of bacteria. In vitro antibacterial activity of LCB01-0183 was tested by the two fold agar dilution method. In vivo activity of LCB01-0183 was determined against systemic infections in mice. LCB01-0183 showed most potent activity among the test compounds against clinical isolates of Gram-positive bacteria. Furthermore, the protective activity of LCB01-0183 was very effective against systemic infections in mice by oral or subcutaneous administration. In time kill study, LCB01-0183 showed a bacteriostatic activity during 24 hours. LCB01-0183 had potent in vitro and in vivo activity against Gram-positive bacteria including drug-resistant strains.

• Bulletin of the Korean Chemical Society
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• v.19 no.7
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• pp.728-730
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• 1998

• Bulletin of the Korean Chemical Society
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• v.14 no.2
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• pp.166-168
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• 1993

• YAKHAK HOEJI
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• v.37 no.5
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• pp.437-441
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• 1993

The efficient synthesis of protected $\beta$-hydroxyhomoserine, which is an important intermediate in the synthesis of Mugineic acid, from cis-2-butene-1, 4-diol as a starting material through 12 steps will be reported herein.

• Archives of Pharmacal Research
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• v.16 no.2
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• pp.158-160
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• 1993

2-Oxazolidinones and 1,3-oxazine-2-ones, key moieties of new antiulcer agents, were prepared successfully by treating corresponding hydroxyamide with N-bromosuccinimide (NBS) and silveracetate in acetonitrile. From the fact that the methods for the preparation of hydoxy amides are versatile and such amides could be converted to the corresponding 2-oxazolid-iones and 1,3-oxazine-2-one under our reaction condition, we think that our method is very practical one for the preparation of such compounds. In addition, the above synthetic example affords a good evidence of the synthetic applicability of our improved Hofmann rearrangement.

• Journal of the Korean Chemical Society
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• v.27 no.6
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• pp.449-456
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• 1983

The facile route of preparing S-2-(${\omega}$-aminoalkylamino) ethyl dihydrogen phosphorothioates, potential chemical radioprotectants, have been studied. Intermediate 3-(2-phthalimidoethyl)-2-oxazolidinone was prepared by a reaction of potassium phthalimide and 3-(2-bromoethyl)-2-oxazolidinone, which was obtained through the alkaline ring closure of a mixture of carbonate and 2,2'-dibromo diethylamine prepared from diethanolamine. This was converted to N-[2-(2-bromoethylamino)ethyl] phthalimide hydrobromide by 30% HBr(gas) in acetic acid and N-(2-bromoethyl)-1,2-ethanediamine dihydrobromide was obtained by reacting the hydrobromide with a solution of HBr-HOAc. N-(2-bromoethyl)-1,3-propanediamine dihydrobromide could be prepared through the Cortese treatment of 2-(3-aminopropylamino) ethanol, which was prepared by a reaction of 1,3-diaminopropane and 2-chloroethanol. These dihydrobromides were treated by sodium thiophosphate in DMF to result S-2-(${\omega}$-aminoalkylamino) ethyl dihydrogen phosphorothioates. The characteristics of each reaction path were discussed in regards to reaction conditions and overall yields and a facile route of preparing each derivative was proposed.