• Title/Summary/Keyword: Oxazolidinone

검색결과 26건 처리시간 0.021초

티오인산이수소 S-2-(${\omega}$-아미노알킬아미노) 에틸들의 간편합성법 연구 (Study on the Facile Preparation of S-2-(${\omega}$-aminoalkylamino) ethyl Dihydrogen Phosphorothioates)

  • 김유선;김석원
    • 대한화학회지
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    • 제27권6호
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    • pp.449-456
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    • 1983
  • 방사선장해를 예방할 수 있는 특성을 지닌 티오인산 이수소 S-2-(${\omega}$-아미노알킬아미노)에틸들의 간편한 합성법을 연구하였다. 중간체인 3-(2-프탈이미도에틸)-2-옥사졸리디논을 프탈이미드 칼륨염과 3-(2-브로모에틸)-2-옥사졸리디논을 반응시켜 만들었으며, 이 브로모에틸의 옥사졸리디논 유도체는 디에탄올아민으로부터 만들어진 2,2-디브로모 디에틸아민과 탄산염 혼합물의 알카리성 고리닫기 반응으로 합성할 수 있었다. 이 중간체는 30% 브롬화수소(가스)-초산용액으로 반응시켜 브롬화수소 N-(2-(2-브로모에틸아미노)에틸)프탈이미드로 유도되었고 이것을 다시 브롬화수소-초산용액으로 반응시켜 이브롬화수소 N-(2-브롬화에틸)-1,2-에탄디아민을 얻을 수 있었다. 1,3-디아미노프로판과 2-클로로에탄올로부터 2-(3-아미노프로필아미노)에탄올을 합성하고 이것을 Cortese씨법으로 처리하여 이브롬화수소 N-(2-브로모에틸)-1,3-프로판아민을 얻었다. 이들 이브롬화수소들을 DMF 용매에서 티오인산 나트륨으로 처리하여 티오인산 이수소 S-2-(${\omega}$-아미노알킬아미노) 에틸들을 합성하였다. 각각의 합성과정의 특징을 반응조건 및 총수율과 관련시켜 논의하였으며 티오인산 유도체를 합성하는 각편한 방법을 제의하였다.

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Synthesis and Antibacterial Activity of Novel 2-Oxo-pyrrolidinyl Oxazolidinones

  • Bhattarai, Deepak;Lee, Sun-Hee;Kim, Hyeong-Kyu;Kang, Soon-Bang;Pae, Ae-Nim;Kim, Eunice Eun-Kyeong;Oh, Taeg-Won;Cho, Sang-Nae;Keum, Gyo-Chang
    • Bulletin of the Korean Chemical Society
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    • 제33권4호
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    • pp.1310-1316
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    • 2012
  • Novel antibacterial oxazolidinones bearing pyrrolidinone ring system at the C-5 side chain were synthesized and their in vitro antibacterial activities were evaluated. Most of the synthesized oxazolidinones showed good antibacterial activity against the Gram-positive and Gram-negative bacteria tested.

Concise Clinical Review of Hematologic Toxicity of Linezolid in Multidrug-Resistant and Extensively Drug-Resistant Tuberculosis: Role of Mitochondria

  • Oehadian, Amaylia;Santoso, Prayudi;Menzies, Dick;Ruslami, Rovina
    • Tuberculosis and Respiratory Diseases
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    • 제85권2호
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    • pp.111-121
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    • 2022
  • Multidrug-resistant tuberculosis (MDR-TB) is caused by an organism that is resistant to both rifampicin and isoniazid. Extensively drug-resistant TB, a rare type of MDR-TB, is caused by an organism that is resistant to quinolone and one of group A TB drugs (i.e., linezolid and bedaquiline). In 2018, the World Health Organization revised the groupings of TB medicines and reclassified linezolid as a group A drug for the treatment of MDR-TB. Linezolid is a synthetic antimicrobial agent in the oxazolidinone class. Although linezolid has a good efficacy, it can cause substantial adverse events, especially hematologic toxicity. In both TB infection and linezolid mechanism of action, mitochondrial dysfunction plays an important role. In this concise review, characteristics of linezolid as an anti-TB drug are summarized, including its efficacy, pathogenesis of hematologic toxicity highlighting mitochondrial dysfunction, and the monitoring and management of hematologic toxicity.

Validation of a Rapid Quantitative Method for the Residues of Nitrofuran Metabolites in Loach by Accelerated Solvent Extraction and HPLC Triple Quadrupole Mass Spectrometry

  • Ryu, Eun Chae;Han, Yun-jeong;Park, Seong-soo;Lim, Chul-joo;Choi, Sunok;Park, Se Chang
    • 한국식품위생안전성학회지
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    • 제31권2호
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    • pp.85-93
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    • 2016
  • 미꾸라지에서의 Nitrofuran계 대사물질인3-amino-2-oxazolidone(AOZ), 5-morpholinomethyl-3-amino-2-oxazolidinone(AMOZ), 1-ammino-hydantoin (AHD)와 semicarbazide(SEM)의 잔류량을 검사하기 위해HPLC-MS/MS를 이용한 신속한 정량법이 개발되었다. 2-nitrobenzaldehyde (2-NBA)를 이용해 $50^{\circ}C$에서 1시간 동안 산 가수분해와 유도체화 과정을 거친 뒤에, 액-액 분배로 정제와 추출을 하였다. 회수율은 음성시료에 3가지 농도 0.5, 1.0, $2.0{\mu}g/kg$의 표준액을 첨가하여 평가하였고 평균 회수율은 75.1-108.1% 이었다. 정밀성(%RSD)은 일내 8.7% 이하, 일간 8.5% 이하였다. 직선성은 NBAOZ는 $0.2-20{\mu}g/Kg$, NBAMOZ는 $0.8-20{\mu}g/Kg$, NBAHD는 $0.2-20{\mu}g/Kg$, NBSEM 는 $0.1-20{\mu}g/Kg$ 범위에서 모두 상관계수 0.99이상이었다. 검출한계(LOD)는 NBAOZ $0.06{\mu}g/Kg$, NBAMOZ $0.24{\mu}g/Kg$, NBAHD $0.06{\mu}g/Kg$, NBSEM $0.03{\mu}g/Kg$이었고, 정량한계(LOQ)는 NBAOZ $0.2{\mu}g/Kg$, NBAMOZ $0.8{\mu}g/Kg$, NBAHD $0.2{\mu}g/Kg$, NBSEM $0.1{\mu}g/Kg$ 이었다. 가수분해 및 유도체화 소요시간을 1시간으로 줄여 만든 신속 간편한 이 시험법이 미꾸라지 중 nitrofuran metabolites잔류량 분석에 적합함을 확인할 수 있었다.

Brief Introduction of Research Progresses in Control and Biocontrol of Clubroot Disease in China

  • He, Yueqiu;Wu, Yixin;He, Pengfei;Li, Xinyu
    • 한국균학회소식:학술대회논문집
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    • 한국균학회 2015년도 춘계학술대회 및 임시총회
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    • pp.45-46
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    • 2015
  • Clubroot disease of crucifers has occurred since 1957. It has spread to the whole China, especially in the southwest and nourtheast where it causes 30-80% loss in some fields. The disease has being expanded in the recent years as seeds are imported and the floating seedling system practices. For its effective control, the Ministry of Agriculture of China set up a program in 2010 and a research team led by Dr. Yueqiu HE, Yunnan Agricultural University. The team includes 20 main reseachers of 11 universities and 5 institutions. After 5 years, the team has made a lot of progresses in disease occurrence regulation, resources collection, resistance identification and breeding, biological agent exploration, formulation, chemicals evaluation, and control strategy. About 1200 collections of local and commercial crucifers were identified in the field and by artificiall inoculation in the laboratories, 10 resistant cultivars were breeded including 7 Chinese cabbages and 3 cabbages. More than 800 antagostic strains were isolated including bacteria, stretomyces and fungi. Around 100 chemicals were evaluated in the field and greenhouse based on its control effect, among them, 6 showed high control effect, especially fluazinam and cyazofamid could control about 80% the disease. However, fluzinam has negative effect on soil microbes. Clubroot disease could not be controlled by bioagents and chemicals once when the pathogen Plasmodiophora brassicae infected its hosts and set up the parasitic relationship. We found the earlier the pathogent infected its host, the severer the disease was. Therefore, early control was the most effective. For Chinese cabbage, all controlling measures should be taken in the early 30 days because the new infection could not cause severe symptom after 30 days of seeding. For example, a biocontrol agent, Bacillus subtilis Strain XF-1 could control the disease 70%-85% averagely when it mixed with seedling substrate and was drenching 3 times after transplanting, i.e. immediately, 7 days, 14 days. XF-1 has been deeply researched in control mechanisms, its genome, and development and application of biocontrol formulate. It could produce antagonistic protein, enzyme, antibiotics and IAA, which promoted rhizogenesis and growth. Its The genome was sequenced by Illumina/Solexa Genome Analyzer to assembled into 20 scaffolds then the gaps between scaffolds were filled by long fragment PCR amplification to obtain complet genmone with 4,061,186 bp in size. The whole genome was found to have 43.8% GC, 108 tandem repeats with an average of 2.65 copies and 84 transposons. The CDSs were predicted as 3,853 in which 112 CDSs were predicted to secondary metabolite biosynthesis, transport and catabolism. Among those, five NRPS/PKS giant gene clusters being responsible for the biosynthesis of polyketide (pksABCDEFHJLMNRS in size 72.9 kb), surfactin(srfABCD, 26.148 kb, bacilysin(bacABCDE 5.903 kb), bacillibactin(dhbABCEF, 11.774 kb) and fengycin(ppsABCDE, 37.799 kb) have high homolgous to fuction confirmed biosynthesis gene in other strain. Moreover, there are many of key regulatory genes for secondary metabolites from XF-1, such as comABPQKX Z, degQ, sfp, yczE, degU, ycxABCD and ywfG. were also predicted. Therefore, XF-1 has potential of biosynthesis for secondary metabolites surfactin, fengycin, bacillibactin, bacilysin and Bacillaene. Thirty two compounds were detected from cell extracts of XF-1 by MALDI-TOF-MS, including one Macrolactin (m/z 441.06), two fusaricidin (m/z 850.493 and 968.515), one circulocin (m/z 852.509), nine surfactin (m/z 1044.656~1102.652), five iturin (m/z 1096.631~1150.57) and forty fengycin (m/z 1449.79~1543.805). The top three compositions types (contening 56.67% of total extract) are surfactin, iturin and fengycin, in which the most abundant is the surfactin type composition 30.37% of total extract and in second place is the fengycin with 23.28% content with rich diversity of chemical structure, and the smallest one is the iturin with 3.02% content. Moreover, the same main compositions were detected in Bacillus sp.355 which is also a good effects biocontol bacterial for controlling the clubroot of crucifer. Wherefore those compounds surfactin, iturin and fengycin maybe the main active compositions of XF-1 against P. brassicae. Twenty one fengycin type compounds were evaluate by LC-ESI-MS/MS with antifungal activities, including fengycin A $C_{16{\sim}C19}$, fengycin B $C_{14{\sim}C17}$, fengycin C $C_{15{\sim}C18}$, fengycin D $C_{15{\sim}C18}$ and fengycin S $C_{15{\sim}C18}$. Furthermore, one novel compound was identified as Dehydroxyfengycin $C_{17}$ according its MS, 1D and 2D NMR spectral data, which molecular weight is 1488.8480 Da and formula $C_{75}H_{116}N_{12}O_{19}$. The fengycin type compounds (FTCPs $250{\mu}g/mL$) were used to treat the resting spores of P. brassicae ($10^7/mL$) by detecting leakage of the cytoplasm components and cell destruction. After 12 h treatment, the absorbencies at 260 nm (A260) and at 280 nm (A280) increased gradually to approaching the maximum of absorbance, accompanying the collapse of P. brassicae resting spores, and nearly no complete cells were observed at 24 h treatment. The results suggested that the cells could be lyzed by the FTCPs of XF-1, and the diversity of FTCPs was mainly attributed to a mechanism of clubroot disease biocontrol. In the five selected medium MOLP, PSA, LB, Landy and LD, the most suitable for growth of strain medium is MOLP, and the least for strains longevity is the Landy sucrose medium. However, the lipopeptide highest yield is in Landy sucrose medium. The lipopeptides in five medium were analyzed with HPLC, and the results showed that lipopeptides component were same, while their contents from B. subtilis XF-1 fermented in five medium were different. We found that it is the lipopeptides content but ingredients of XF-1 could be impacted by medium and lacking of nutrition seems promoting lipopeptides secretion from XF-1. The volatile components with inhibition fungal Cylindrocarpon spp. activity which were collect in sealed vesel were detected with metheds of HS-SPME-GC-MS in eight biocontrol Bacillus species and four positive mutant strains of XF-1 mutagenized with chemical mutagens, respectively. They have same main volatile components including pyrazine, aldehydes, oxazolidinone and sulfide which are composed of 91.62% in XF-1, in which, the most abundant is the pyrazine type composition with 47.03%, and in second place is the aldehydes with 23.84%, and the third place is oxazolidinone with 15.68%, and the smallest ones is the sulfide with 5.07%.

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일개 대학병원의 임상 검체에서 분리한 포도알균 항생제 내성 경향 차이 (Differences in the Antibiotic Resistance Pattern of Staphylococcus aureus Isolated by Clinical Specimens in a University Hospital in South Korea)

  • 홍성노;김준;성현호
    • 대한임상검사과학회지
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    • 제50권2호
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    • pp.85-92
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    • 2018
  • 황색포도상구균의 유병률에 대한 정보와 항생제 내성 리스트는 전 세계 어느 곳에서나 황색포도상구균 감염의 적절한 치료 방법을 선택하는 데 필요하다. 이 연구는 한국의 어느 병원 임상 검체에서 얻은 황색포도상구균 균주의 빈도와 항생제 저항성을 조사하기 위하여 수행하였다. 그람 양성구균 1,746 개의 균은 S. aureus으로 확인되었다. S. aureus은 객담(N=565, 32.4%), 기관내 흡인(358, 20.5%), 상처(329, 18.8%), 혈액(137명, 7.8 %), 고름(59 %, 3.4 %)이었다. 객담, 기관 내 흡인, 상처, 혈액, 소변 및 고름에서 스크리닝 된 1,282개의 S. aureus 균주 모두 글리코 펩타이드 옥시 졸리 디논(리네 졸리드) 및 스트렙토그라민(퀴뉴프리스틴/달포프리스틴)에서 모두 민감성이 나타났다. 황색 포도상 구균은 기관 내 흡인과 비교하면 소변, 혈액, 고름, 상처 및 객담에서 내성이 유의하게 낮았으며(P<0.01), 기관내 흡인 검체에서 분리 된 황색포도상 구균의 경우 특히 내성의 빈도가 높았다. 결과적으로, 임상 표본에 따라 황색 포도상 구균의 항생제 저항성에는 상당한 차이가 있었다.