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6-Exomethylene penamsulfone 유도체의 β-lactamase 저해작용
김해종,여성현,임채욱,임철부,김미영 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-
6-Exomethylene penam derivatives were tested as possible β-lactamase inhibitors. The in vitro β-lactamase inhibitory activities were determined by a spectrophotometric assay using Type Ⅰ, Ⅱ, Ⅲ, Ⅳ and TEM β-lactamase. Their activities were compared with sulbactam, tazobactam and clavulanic acid. The 6-exomethylene sulfone derivatives were more potent than clavulanic acid and sulbactam against Type Ⅳ β-lactamase. The Z-isomers showed stronger activities than the E-isomers against TEM and Type Ⅳ β-lactamase.
임철부,이인숙,임채욱 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-
In order to find new antimicrobial agents, twelve new alkylene bis benzothiazolyl biguanides and eight benzothiazoly biguanides were synthesized. The treatment of alkylenediamines·2HCI with sodium dicyanamide afforded alkylene bis cyanoguanidines. Alkylene bis benzothiazolyl biguanides were synthesized by the reaction of alkylene bis cyanoguanidines with 2-aminobenzothiazole. Benzothiazolyl biguanides were obtained from N-cyanoheterocyclylamidines and 2-aminobenzothiazoles through the similar procedures.
Benzothiazolyl Biguanides의 항미생물작용
임철부,이인숙,임채욱 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-
The twenty benzothiazolyl biguanides synthesized were evaluated for their antimicrobial activities against Staphylococcus aureus. Bacillus subtilis, Mycobacterium phlei, Escherichia coli, Microsporium canis, Candida albicans, Sporothrix schenkii and Trichophyton mentagrophytes. The results obtained were as follow : The most active compound, 1,6-bis{N^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido} hexane·2HCI (14) showed the growth inhibitory activity against S. aureus at the concentration of 7.81ug/mL, against B.subtilis at 15.63ug/mL and against M. phlei at 31.25ug/mL. 1,6-Bis {N^5-(6-chlorobenzothiazol-2-yl)-N^1-biguanido} hexane·2HCI(14), 1,6-Bis{N^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido) hexane·2HCI (15) and N-(6-chlorobenzothiazol-2-yl)-1-piperidinylamidinoamidine·HCI (24) inhibited the growth of M. phlei at the concentration of 31.25ug/mL respectively. 1,4-Bis{N^5-(6-methylbenzothiazol-2yl)-N^1-biguanido}butane·2HCI(9) and 1,4-bis{N^5-(6-bromobenzothiazol-2-yl)-N^1-biguanido}butane·2HCI(11) exhibited the antimicrobial activity against B.subtilils at the concentration of 31.25ug/mL. Twelve new biguanide compounds showed growth inhibitory activities against C. albicans at the concentration of 400ug/mL.
β-Lactamase생성균주에 대한 새로운 β-Lactamase Inbitating Compound와 β-lactam항생제와의 병용시 항균효과
홍인표,김홍진,임채욱,김기호 중앙대학교 약학연구소 1996 약학 논총 Vol.10 No.-
The in vitro and in vivo activities of CH1250, a new β-lactamase inhibiting compound, were compared with the activities of clavulanic acid and sulbactam against 30 β-lactamase-producing bacteria. Broth microdilution susceptibility testing was performed to compare the activities of β-lactamase inhibitors. Serial two fold dilutions of β-lactams were tested alone and in two combinations with β-lactamase inhibitor. CH1250 was more active than clavulanic acid against Acinetobacter calcoaceticus S21, Pseudomonas aerug-nosa GN918, Proteus vulgaris 20, Staphylococcus aureus MS15009/1258, Serratia marcescens 1 when combined with cefotaxime. When combined with amoxicillin, CH1250 was more effective against Citrobacter diversus 2046E. Staphylococcus aureus MS25009/1258, Proteus vulgaris GN76. With ampicillin, CH1250 had an better or simillar activities against Escherichia coli 3455E, Klebsiella aerogenes 1976E, Serratia marcescens 1, Staphylococcus aureus MS15009/1258. The efficacy of ampicillin-CH1250 in treatment of mice with systemic infections produced by Klebsiella aerogenes 1976E, a β-lactamase-producing bacteria, was compared with that of ampicillin, ampicillin-sulbactam. Acute systemic infections in mice were produced by i.p. inoculation of bacterial cultures suspended in 6% mucin. Mice were treated s.c. 1hr after challenge. PD50s of the ampicillin, ampicillin-sulbactam. ampicillin-CH1250 were 334.32, 170.58, 250.5mg/kg, respectively. CH1250 was not more effective than sulbactam in reducing ampicillin doses required to protect mice from infection produced with Klebsiella aerogenes 1976E. The reduction in the 50% protective dose of ampicillin by CH1250 was 23% better than those effected by sulbactam for Klebsiella aerogenes 1976E infection.
Im, Chae-Uk,Yim, Chul-Bu,Oh, Jung-Suk,Yoon, Sang-Bae The Pharmaceutical Society of Korea 1997 Archives of Pharmacal Research Vol.20 No.6
The 6, 6-dibromopenam 6 was treated with $CH_{3}/MgBr$ and carbaldehyde 5 to afford the 6-bromo-6-(1-hydroxy-1-methyl)penicillanate 7, which was reacted with acetic anhybride to give acetoxy compound 8. The deacetobromination of 8 with zinc and acetic acid gave 6-exomethylenpenams, Z-isomer 9 and E-isomer 10, which were oxidized to sulfones 11 and 12 by m-CPBA. The p-methoxybenzyl compounds were deprotected by $AlCl_{3}$ and neutralized to give the sodium salts 13, 14, and 15.
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),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.
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.
( Hyung Uk Jeong ),( Hyun Hwak Im ),( Sung Kwon Chang ),( Chae Hoon Paik ),( Tae Ho Han ),( In Seon Kim ),( Ik Soo Kim ) 한국잠사학회 2007 International Journal of Industrial Entomology Vol.15 No.1
A diverse kind of environment-friendly agricultural materials (EFAM) for the control of insect pests is on the market. These EFAMs are a part of essential sources for the accomplishment of successful, sustainable, and environment-friendly agriculture. Thus, accurate information of these EFAMs is one that required for the success of environment-friendly agriculture, but, in reality, still appropriate information is absolutely in shortage. In this study, we, therefore, tested the efficacy of commercial EFAMs against two lepidopteran insect larvae, the diamondback moth Plutella xylostella (Lepidoptera: plutellidae) and the tobacco cutworm Spodoptera litura (Lepidoptera: Noctuidae). After the two insect pests were successfully stabilized in indoor environment the larvicidal activity was tested at 24±1°C, relative humidity (RH) of 60±5%, and a photoperiod of 16L : 8D, and mortality was determined 48 hrs after EFAMs are treated. The EFAMs that showed more than 90% of larvicidal activity were each six among 16 against both R xylostella and S. litura and only three of them showed consistent larvicidal activity against both species, signifying species specificity of EFAMs and importance of selection of proper EFAMs depending on target insect pest.