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6-Exomethylenepenam유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교
임채욱,박희석,정미량,강주성,임철부 대한약학회 2003 약학회지 Vol.47 No.6
In vitro $\beta$-lactamase inhibitory activity of 6-exomethylenepenam compounds ( 1, 2, 3, 4 and 5) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of compound 3 was stronger than those of sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III, IV, TEM enzymes. The inhibitory activity of 5 was stronger than sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III, and IV enzymes. The in vitro antimicrobial activity of 3, 4 and 5 combined with ampicillin and cefoperazone was compared with the sulbactam against $\beta$-lactamase producing 27 strains. But, synergistic activity of 3 and 5 was inferior to tazobactam.
임채욱,권오혁,홍용기,임철부 중앙대학교 약학연구소 2001 약학 논총 Vol.15 No.-
Five indomethacin amides as potential nonsteroidal analgesic and antiinflammatory compounds were prepared. Indomethacin and hydroxysuccinimide were reacted with dicyclohexyl carbodiimide to give indomethacin active ester (4), which was treated with amines to yield indomethacin amides (5-9).
임채욱,박상민,홍용기,임철부 중앙대학교 약학연구소 2001 약학 논총 Vol.15 No.-
Six Aryl acetic acid amides as potential nonsteroidal analgesic and antiinflammatory compounds were prepared. Cinmetacin and indomethacin were reacted with dicyclohexyl carbodiimide and hydroxysuccinimide to give active ester (4-5), which was treated with amines to yield indomethacin amides (6-11).
(4-Nicotinate-2-yl)thiobutyl 6-Exomethylene Penam의 합성
임채욱,박희석,임철부 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-
The synthesis of new 6-exomethylene penam containing triazole ring was described. 1, 3-Dipolar cycloaddition of 4-azidobutanol with propargyl aldehyde gave 1-(4-hydroxybutyl)-1,2,3-triazole-4-carboxaldehyde, which reacted with 6,6-dibromopenicillanate to yield the stereoisomeric mixture of 6-bromo -6-〔hydroxy-1-(triazol-4-yl)methyl〕 penicillanate compound. This hydroxy compound was treated with acetic anhydride and zinc to afford the 6-exomethylene penam compound.
임채욱,이극선,오옥희,이현수,임철부 중앙대학교 약학연구소 2000 약학 논총 Vol.14 No.-
The 15 synthesized p-aminosalicylate esters derivatives were evaluated for their antimicrobial activities, in vitro, against Mycobacterium phlei (CACC 75432), Staphylococcus aureus (CHA 78311), Bacillus subtilis (CAUCC 310) and Escherichia coli (P32). Bivalent ligand derivatives (1-6) showed weaker activities than their parent p-aminosalicylate(PAS) in vitro. But some of thiouera derivatives (8 and 10) gave stronger activities against Mycobacterium phlei and Staphylococcus aureus than their parent p-aminosalicylate.
N,N'-Succinyl bis(p-Aminosalicylate) 유도체의 합성
임채욱,이극선,유재학,이현수,임철부 중앙대학교 약학연구소 2000 약학 논총 Vol.14 No.-
The synthesis of bivalent ligand derivatives of p-aminosalicylate derivatives was described. p-Aminosalicylate was reacted with alcohols to give esters, which was treated with succinyl chloride to yield N,N'-bis(p-aminosalicylate) under Schotten-Baumann condition. The treatment of succinyl chloride with glycine and then reacted with N-hydroxysuccinimide, DCC, and N,N'-bis(p-aminosalicylate) gave N,N'-succinyl bis(p-glycylamino salicylate) derivatives.