• Title/Summary/Keyword: antibacterial agents

Search Result 384, Processing Time 0.035 seconds

Synthesis and Biological Valutaion of New 5-Fluorobenzimidazole Antifungal Agents (새로운 5-Fluorobenzimidazole 항진균제의 합성과 생물학적 평가)

  • Ryu, Soung-Ryual
    • Journal of the Korean Applied Science and Technology
    • /
    • v.28 no.1
    • /
    • pp.118-125
    • /
    • 2011
  • New type of 5-fluorobenzimidazole derivatives was synthesized through the reaction of 4-fluoro-5-(2,6-dimethylmorpholinyl)-2-aminoaniline with 5-nitro-2-furoic acid and 5-methoxy-3-chlorobenzothiophene-2-carboxylic acid in presence of PPA and treatment of $OH^-$. the resulting substituted 5-fluorobenzimidazole derivatives(6), (7) was characterized by high solubility in common polar organic solvents. We considered 5-fluorobenzimidazole derivatives were useful especially for antifungal drugs. These results are discussed from the viewpoints of the chemical and physical structures of the 5-fluorobenzimidazole derivatives.

Carrier-Mediated Tissue Distribution and Blood-Brain Barrier Transport of New Quinolones

  • Tsuji, Akira
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1997.04a
    • /
    • pp.57-63
    • /
    • 1997
  • Animal and clinical investigations have shown that fluoroquinolones, new quinolone antibacterial agents (NQs), are well absorbed across the intestinal tract, with a bioavailability of 60-90% after oral administration. Although some types of carrier-mediated intestinal transport mechanisms have been reported for enoxacin (ENX), ofloxacin (OFLX) and sparfloxacin (SPFX), recent results using a human intestinal epithelial cell line, Caco-2, indicated a passive or nonsaturable transport of SPFX, one of the most hydrophobic NQs. The mechanism underlying the intestinal absorption of NQs is still largely unknown. The distribution of NQs into peripheral tissues including erythrocytes is very rapid and their tissue-to-plasma concentration ratios (Kp) are considerably larger than those of inulin (an extracellular fluid space marker), in spite of almost complete ionization of NQs at the physiological pH. Our findings suggest that OFLX and lomefloxacin (LFLX) are taken up by rat erythrocytes via a transport system common to that of a water-soluble vitamin, nicotinic acid.

  • PDF

Synthesis and Antimicrobial Activity of Novel Tetrahydrobenzothienopyrimidines

  • Amal Abdel Haleem Mohamed Eissa;Ashraf Ahmed Moneer
    • Archives of Pharmacal Research
    • /
    • v.27 no.9
    • /
    • pp.885-892
    • /
    • 2004
  • Due to the rapidly growing number of resistant strains of bacteria, the search for antibacterial agents with new modes of action will always remain an important and challenging task. Thus, the reaction of 2-substituted or. unsubstituted-4-(4-acetylanilino)-5,6,7,8-terahydrobenzo[b] thieno[2,3-d]pyrimidine derivatives 1-3 with the hydrazine derivatives, semi and / or thiosemi-carbazides, provided the corresponding hydrazones 4-6 and semi and/or thiosemicarbazones 7-9. Claisen-Schmidt condensation of compounds 1 or 2 with the appropriate aldehyde yielded the chalcones 10, 11 which, when treated with hydroxylamine hydrochloride gave rise to the isoxazoline-containing compounds 12, 13. Furthermore, reacting the respective chalcones 10, 11 with different hydrazines, urea and/or thiourea, furnished compounds 14, 15, 16, and 17 respectively. Representative compounds were tested for their antimicrobial activity against Candida Albicans and certain gram-positive and gram-negative bacteria. Their MICs were then determined. Compound 15e, showed a broad spectrum of activity while most of the other com-pounds showed varying antimicrobial activity.

Photocleavage of DNA by 4′-Bromoacetophenone- Pyrrole Carboxamides

  • Jeon, Raok
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 2001.11a
    • /
    • pp.79-79
    • /
    • 2001
  • Genotoxic chemotherapeutics are irreversible DNA targeting agents, which can act as anticancer and antiviral drugs. Natural antibacterial and anticancer enediynes function through the formation of free radicals formed by Bergman-type cycloaromatization and being capable of cleavage of DNA strand. They have been focused primarily on the design and syntheses of simple enediyne structures, which can be mimic their mechanistic feature. Recently. I have been reported the possible application of 4'-bromoacetophenone as a simple photoactivatable DNA cleaving agent, which could be readily prepared and exhibit potent and selective DNA cleaving activity. Herein, we further investigated the activity of 4'-bromoacetophenone-pyrrolecarboxamides, which consist of both DNA cleaving element and recognition unit under various conditions in order to get more understanding of the mechanism of the action and find a broad spectrum of application.

  • PDF

Studies on the Volatile Oil Constituents in Artemisia sp. -Isolation and Determination of Camphor by Gas Chromatography- (Artemisia 속 정유 성분에 관한 연구 -Gas Chromatography에 의한 Camphor의 분리 및 정량-)

  • Hahn, Dug-Royng;Kim, Ihn-Hae
    • Korean Journal of Pharmacognosy
    • /
    • v.4 no.2
    • /
    • pp.71-74
    • /
    • 1973
  • The contents of volatile oil and camphor in the oil of Artemisia messer-schmidtiana $B_{ESSER}$ var. viridis $B_{ESSER}$ f. typica $N_{AKAI}$ and Artemisia asiatica $N_{AKAI}$ which were known to be effective as antibacterial, antifungal and antineoplastic agents by screening experimentation, were determined quantatively by gas chromatography. The volatile oil contents of Artemisia messer-schmidtiana $B_{ESSER}$ var. viridis $B_{ESSER}$ f. typica $N_{AKAI}$ and Artemisia asiatica $N_{AKAI}$ are 0.17% and 0.19%, and the camphor contents are 8.51% and 1.46%, respectively.

  • PDF

Cordycepin: pharmacological properties and their relevant mechanisms

  • Baoyan, Fan;Haibo, Zhu
    • CELLMED
    • /
    • v.2 no.2
    • /
    • pp.14.1-14.7
    • /
    • 2012
  • Cordycepin, a nucleoside derivative, was extracted from $Cordyceps$ $sinensis$, and then proved to be a bioactive compound present in traditional Chinese medicine Cordyceps. Early investigations revealed cordycepin possessed anti-microbial activity mainly by inhibiting nucleic acid synthesis. Although cordycepin is not used as antibacterial agents in clinic, its other pharmacological effects and possible mechanisms have gradually been deeply studied. This review serves to summarize the research progress of cordycepin.

Cultural characterization of probiotic Lactobacillus sakei BK19

  • Yang , Byung Gyoo;Song , Choon Bok;Yeo , In Kyu;Lee , Kyoung Jun;Park , Geun Tae;Lee, Sang Hyeon;Son, Hong Joo;Heo, Moon Soo
    • Journal of fish pathology
    • /
    • v.16 no.2
    • /
    • pp.119-123
    • /
    • 2003
  • We have selected an valuable pmbiotic strain; Lactobacillus sakei BK19 which has wide antagonic spectrum against fish pathogens . Present study investigated cultural characterization of L. sakei BK19 including pH tolerance , susceptibility of antibacterial agents and growth pattern with different environment such as nutritions, temperature and salinity. L. sakei BK19 showed Significantly higher resistance at low pH(around pH 4) environment and relative high antibiotic tolerance . In the study of optimal culture condition, maltose and saccharose provided the optimal nutritional culture condition while lactose and mannitol were unable to supply its carbon source for the fermentation of L. sakei BK19. Moreover. L. sakei BK19 showed good growth at the temperature range of 15 to $45^{o}C$ und the NaCl concentration of 0 to 7%. Hence, this particular probiotic strain may be benificial both in seawater and fresh weter conditions.

Analysis of Genetic Diversity of Bifidobacterium spp. Isolated from Korean Adults Fecal Samples (한국 성인 분변 시료에서 분리한 비피더스균의 유전자 다양성 분석)

  • 배학균;김선옥;박종선;강병용;최성숙;강진양;하남주
    • YAKHAK HOEJI
    • /
    • v.48 no.1
    • /
    • pp.20-26
    • /
    • 2004
  • Twelve strains of Bifidobacterium spp. were isolated from the feces of healthy Korean 20∼30 years. The identification of genera from isolates were performed by the microscopic observation and fructose-6-phosphate phosphoketolase (F6PPK) activity which is the key enzyme to distinguish the Bifidobacterium spp. from other anaerobic bacteria. To determine the antibacterial resistance patterns, minimum inhibitory concentration (MIC) of several antibiotics (including anti-tuberculosis agents) was determined. Five of the isolate!, showed the high degree of resistance to vancomycin. To investigate the genetic diversity between isolates and type strain of Bifidobacterium spp. from KCTC, we peformed the RAPD-fingerprinting. Using a total set of four primers, it is possible to distinguish the isolates and Bifidobacterium spp. from KCTC. Thus, Bifidobacterium strains isolated from our samples may be a new species or strains of Bifidobacteriurn genera, and have the potential as a probiotics.