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임채욱(Chae Uk Im),박희석(Hee Suk Park),이현수(Hyun Soo Lee),임철부(Chul Bu Yim) 대한약학회 2000 약학회지 Vol.44 No.2
The synthesis of new 6-exomethylene penams with triazole ring was described. The 6,6-dibromopenam 5 was treated with CH3MgBr and carbaldehyde 4 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 6, which was reactod with acetic anhydride to give acetoxy compound 7. The deacetobromination of 7 with zinc and acetic acid gave 6-exomethylenpenams, Z-isomer 8 and E-isomer 9, which were oxidized to sulfones 10 and 11 by m-CPBA. The p-methoxybenzyl compounds 6~11 were deprotected by AlCl3 and neutralized to give the sodium salts 12~17.
Sulbactam 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교
임채욱(Chae Uk Im),박희석(Hee Suk Park),김용현(Yong Hyun Kim),임철부(Chul Bu Yim) 대한약학회 2002 약학회지 Vol.46 No.6
In vitro β-lactamase inhibitory acclivity of 6-exomethylene sulbactam compounds (CH-120,130,140,145,150, 155) was compared with calvulanic acid, sulbactam and taaobactam. The inhibitory activity of CH-140 was stronger than surfbactam and davulanic acid against Type II, III, IV, TEM enzymes and stronger than tazobactam against Type IV enzyme. The inhibitory activity of CH-145 was stronger than sulbactam and clavulanic acid against Type I, II, III, IV, TEM enzpnes and stronger than tasobactam against Type III, IV enzymes. The in vitro antimicrobial activity of CH-140 and CH-145 combined with piperaciBlin and ceftriaxone was compared with the sulbactam and taaobactam against β-1actamase producing 31 strains. But Synergistic activity of CH-140 and CH-145 was inferior to tazobactam.
임채욱(Chae Uk Im),정홍식(Hong Sik Jeong),임철부(Chul Bu Yim) 대한약학회 2002 약학회지 Vol.46 No.6
The synthesis of new 6-ex(nnethylene sulbactam derivatives with 5-methyl-1,3,4- thiadiazole was described. The 6,6-dibromopenam 5 was reacted with CH3MgBr and carbaldehyde 4 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 6, which was treated with acetic anhydride to give acetoxy compound 7. The deacetobromination of acetoxr compound 7 with zinc and acetic acid gave 6-exomethylen penams, Z-isomer 8 and E-isomer 9, which was oxidiged to sulfones 10 by m-CPBA. The p- methoxybenzyl compounds 6-10 were deprotected by AIC13 and neutralized with NaOH solution to give the sodium salts 11-15.
6-벤조치아졸 페니실린 유도체의 베타락타마제 효소억제력과 베타락탐항생제 병용시 활성비교
윤상배,임채욱,Yoon, Sang-Bae,Im, Chae-Uk 대한약학회 2008 약학회지 Vol.52 No.4
In vitro ${\beta}-lactamase$ inhibitory activity of 6-benzothiazole penicillins (1, 2, 3 and 4) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of exomethylene compounds (3 and 4) was stronger than those of non-exomethylene compounds (1 and 2). The sulfide 3 showed stronger inhibitory activity than sulbactam, clavulanic acid andsimilar to tazobactam against ${\beta}-lactamase$ Type I enzymes. The inhibitory activity of 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type III and IV enzymes. The in vitro antimicrobial activity of ampicillin or cefoperazone combined with 3 or 4 was stronger than those of ampicillin or cefoperazone alone against many ${\beta}-lactamase$ producing strains to show that compounds 3 and 4 have some synergistic effect. The synergistic activity of 3 and 4 was comparable to sulbactam in some ${\beta}-lactamase$ producing strains, but it was inferior to tazobactam.
혼성 Bivalent Ligand 퀴놀론 유도체의 합성
이상필,임채욱,김동순,임철부,Lee, Sang-Pil,Im, Chae-Uk,Kim, Dong-Soon,Yim, Chul-Bu 대한약학회 1994 약학회지 Vol.38 No.6
Eighteen new hybrid bivalent ligand quinolones that contain two different type of pharmacophores in a single molecule were prepared and evaluated for in viかo antibacterial activity. Hybrid bivalent ligands p-nitrobenzyloxycarbonyl quinolones were prepared by the treatment of active esters of succinyl fluoroquinolones with 1,7-disubstituted fluoroquinolone carboxylic acids in DMF. Eighteen final quinolone carboxylic acids were obtained by the reduction of compounds $25{\sim}42$ with hydrogen in the presence of 10% Pd-C. Among these derivatives, compound[56] showed the most potent antibacterial activity against a wide range of microoranisms.
${\beta}-Lactamase$ 억제작용이 기대되는 7-Arylidene Cephalosporanate 유도체의 합성
이종민,임철부,임채욱,Lee, Jong-Min,Yim, Chul-Bu,Im, Chae-Uk 대한약학회 2008 약학회지 Vol.52 No.4
The synthesis of 7-arylidene cephalosporanates for ${\beta}-lactamase$ inhibitor was described. The reactions of substituted benzyl halides $[1]{\sim}[3]$ with triphenylphosphine gave triphenylphcsphonium chlorides $[4]{\sim}[6]$. These phosphonium salts were treated with n-butyllithium to give ylides, which were reated with 7-oxocephalosporanate [7] by Wittig reaction to afford the 7-exomethylene cephalosporanates $[8]{\sim}[10]$. These cephalosporanates were oxidized to cephalosporanate sulfones $[11]{\sim}[13]$ with mCPBA. The deprotection of benzhydryl cephalosporanate $[8]{\sim}[13]$ with $AlCl_3$ and $NaHCO_{3}$ gave sodium salts of 7-arylidene cephalosporanates $[14]{\sim}[19]$.
N- 치환 Glycyl Norfloxacin 유도체의 합성과 항균작용
이현수(Hyun Soo Lee),임채욱(Chae Uk Im),임철부(Chul Bu Yim) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.2
The synthesis and antimicrobial activity of N-substituted glycyl derivatives of Norfloxacin were described. Norfloxacin was treated with chloroacetyl chloride to yield chloroacetyl norfloxacin (1). This compounds was reacted with alkyldiamines to afford bivalent ligand quinolone carboxylic acids (2-6), which was added to pivaloyloxymethyl chloride to give bivalent ligand pivaloyloxymethyl quinolone carboxylates (7-11). Chloroacetyl norfloxacin (1) treated with alkylamines to obtain monovalent ligand quinolone carboxylic acids (12-15), which was reacted with pivaloyloxymethyl chloride to get monovalent ligand pivaloyloxymethyl quinolone carboxylates (16-19). Free carboxylic quinolones (2-6, 12-15) showed little stronger activities to their pivaloyloxymethyl esters (7-11, 16-19). In monovalent ligand quinolone analogues, longer alkyl chain compounds showed stronger activities than shorter one.
6위치 엑소 메칠렌 치환 페남계 베타락타마제 억제제의 베타락탐항생제와 병용시 활성비교(I)
박계환(Kye Whan Park),김기호(Ki Ho Kim),김미영(Mee Young Kim),임채욱(Chae Uk Im),임철부(Chul Bu Yim) 대한약학회 1997 약학회지 Vol.41 No.4
In this approach, the antimicrobial activities of the compounds were compared with the beta-lactam antibiotics against beta-lactamase producing strains in vitro. Heterocyclyl exomethylenepenam derivatives were several numbers of 6-exomethylenepenam sodiums (CH1240, CH1245, CH1250, CH2140, CH2145, CH2150). The inhibitory concentraion assay of six compounds were compared with clavulanic acid, sulbactam, tazobactam. Clavulanic acid, sulbactam and tazobactam are used as inhibitors of a variety of plasmid-mediated beta-lactamases. In vitro beta-lactamase inhibitory assay, CH1240 and CH2140 were more active than clavulanic acid, sulbactam and tazobactam against beta-lactamases overally. And in vitro comparative antimicrobial susceptibility test of six inhibitors were performed with mixed forms of ampicillin, cefotaxime, amoxicillin, ticarcillin, piperacillin, cefoperazone against beta-lactamase producing 31 species strains. Consequently CH2140 and CH1240 among the six compounds enhanced the activity of the beta-lactams for 31 beta-lactamase producing strains.
7-엑소메칠렌 세팔로스포라네이트 유도체의 합성과 beta-락타메이즈 억제작용
이종민(Jong Min Lee),최수항(Su Hang Choi),이현수(Hyun Soo Lee),임채욱(Chae Uk Im),임철부(Chul Bu Yim) 대한약학회 1999 약학회지 Vol.43 No.6
7-Oxocephalosporanate 1 was treated with phosphonium salts 2~4 by Wittig reaction to afford 7-exomethylene cephalosporanates 5-7. They were oxidized to sulfones 8-10 with mCPBA. Deprotection of benzhydryl 7-exomethylene cephalosporanate with AlCl3 and NaHC03 gave sodium salts of 7-exomethylene cephalosporanates 11-16. The beta-lactamase inhibitory activity of synthesized compounds 11~16 were compared with sulbactam, tazobactam and clavulanic acid against Type I, II, III, IV and TEM-2 beta-lactamase in vitro. Compound 15 showed more potent activity than sulbactam and clavulanic acid against Type III, IV beta-lactamase enzyme.
Monovalent와 bivalent aminoantipyrine 유도체의 합성과 항염 진통활성
김승재(Seung Jae Kim),권오혁(Oh Hyeok Kwon),전상철(Sang Chul Jun),박상민(Sang Min Park),임채욱(Chae Uk Im),임철부(Chul Bu Yim) 대한약학회 2002 약학회지 Vol.46 No.3
Six novel 4-aminoantipyrine derivatives as potential nonsteroidal antiinflammatory and analgesic compounds were prepared and their antiiflammatory-analgesic activity were compared with antipyrine. Succinyl chloride and Ac20 were reacted with glycine, respectively to give glycine compounds (3-4, 9-10), which were treated with hydroxysuccinimide and dicyclohexyl carbodiimide to yield active esters (5-6,11-12), and then reacted with 4-aminoantipyrine to prepare 4-aminoantipyrine derivatives (7-8, 13-14). 4-Aminoantipyrine reacted with succinyl chloride and Ac20, respectively to give succinyl leis aminoantipyrine (15) and acetyl aminoantipyrine (16). Compounds (7), (8) and (13) gave comparable antiinflammatory activity to antipyrine.