抗菌药(英文PPT)Antimicrobials
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抗菌药精品PPT课件
• 药物设计中的前药
– 降低毒性刺激性 – 改善吸收分布代谢排泄性质 – 延长半衰期 – 形成组织特异性 – 提高稳定性
4.2.2主要药物和基本结构
1.主要药物
2.基本结构
Sulfadiazine, SD 磺胺嘧啶 P78 下二
对位取代的氨基苯磺酰胺结构是 活性必须的
Sulfamethoxazole, SMZ 磺胺甲噁唑 P79 上一（新诺明）
• 设计与生物体内基本代谢物结构相似的化 合物，干扰基本代谢物的吸收、合成、利 用
• 常用于化学治疗药的设计 • 基本代谢物：叶酸、核酸、碱基、脂质
4.2.3 磺胺甲噁唑
被氧化
理化性质
被水解
碱性
酸性
乙酰化
1.水中不溶解，但表现酸碱两 性，在盐酸氢氧化钠等中可溶 解 2.可水解、氧化，保存需避免 潮湿 3.体内可乙酰化，影响溶解度 形成尿路结石
• 先导化合物对给定的靶标要呈现一定的活 性、选择性；同时符合类药性，具有可开 发性
• 先导化合物因为活性、安全性、药代动力 学性质等因素不能成为药物
• 先导化合物的发现和优化是药物化学的重 要任务
先导化合物的发现
• 磺胺类——基于筛选发现先导化合物（磺 胺米柯定）
• 磺胺类——从代谢产物发现先导化合物 （对氨基苯磺酰胺）
4.3.2 喹诺酮类药物的发展
• 萘啶酸是第一个喹诺 酮类抗菌药
• 1962年合成，第一代 喹诺酮
• 抗菌谱较窄，对G-中 等活性，对G+和绿脓 杆菌无作用
从现有药物的合成副产物 中发现先导化合物
Nalidixic acid 萘啶酸 P70 上二
先导化合物 Lead compoud P551
先导化合物 Lead Compound
– 降低毒性刺激性 – 改善吸收分布代谢排泄性质 – 延长半衰期 – 形成组织特异性 – 提高稳定性
4.2.2主要药物和基本结构
1.主要药物
2.基本结构
Sulfadiazine, SD 磺胺嘧啶 P78 下二
对位取代的氨基苯磺酰胺结构是 活性必须的
Sulfamethoxazole, SMZ 磺胺甲噁唑 P79 上一（新诺明）
• 设计与生物体内基本代谢物结构相似的化 合物，干扰基本代谢物的吸收、合成、利 用
• 常用于化学治疗药的设计 • 基本代谢物：叶酸、核酸、碱基、脂质
4.2.3 磺胺甲噁唑
被氧化
理化性质
被水解
碱性
酸性
乙酰化
1.水中不溶解，但表现酸碱两 性，在盐酸氢氧化钠等中可溶 解 2.可水解、氧化，保存需避免 潮湿 3.体内可乙酰化，影响溶解度 形成尿路结石
• 先导化合物对给定的靶标要呈现一定的活 性、选择性；同时符合类药性，具有可开 发性
• 先导化合物因为活性、安全性、药代动力 学性质等因素不能成为药物
• 先导化合物的发现和优化是药物化学的重 要任务
先导化合物的发现
• 磺胺类——基于筛选发现先导化合物（磺 胺米柯定）
• 磺胺类——从代谢产物发现先导化合物 （对氨基苯磺酰胺）
4.3.2 喹诺酮类药物的发展
• 萘啶酸是第一个喹诺 酮类抗菌药
• 1962年合成，第一代 喹诺酮
• 抗菌谱较窄，对G-中 等活性，对G+和绿脓 杆菌无作用
从现有药物的合成副产物 中发现先导化合物
Nalidixic acid 萘啶酸 P70 上二
先导化合物 Lead compoud P551
先导化合物 Lead Compound
抗微生物药物英文PPTAntimicrobial
Figure 20.9
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Polypeptide antibiotics
– Bacitracin
• Topical application • Against gram-positives
– Gram-positives
• Binds 50S, prevents translocation
• Oxazolidinones
– Linezolid
• Gram-positives
– Binds 50S subunit, prevents formation of 70S ribosome
Figure 20.12
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
Figure 20.8
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Cephalosporins
– 2nd, 3rd, and 4th generations more effective against gramnegatives
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B
– Topical – Combined with bacitracin and neomycin in
– Changes shape of 30S subunit
Antibacterial Antibiotics Inhibitors of Protein Synthesis
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Polypeptide antibiotics
– Bacitracin
• Topical application • Against gram-positives
– Gram-positives
• Binds 50S, prevents translocation
• Oxazolidinones
– Linezolid
• Gram-positives
– Binds 50S subunit, prevents formation of 70S ribosome
Figure 20.12
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
Figure 20.8
Antibacterial Antibiotics Inhibitors of Cell Wall Synthesis
• Cephalosporins
– 2nd, 3rd, and 4th generations more effective against gramnegatives
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B
– Topical – Combined with bacitracin and neomycin in
– Changes shape of 30S subunit
Antibacterial Antibiotics Inhibitors of Protein Synthesis
抗生素英文课件精品——Antimicrobial Drugs
Ch 20: Antimicrobial Drugs
• Chemotherapy • Antimicrobial drugs • Antibiotic
• Selective toxicity
The use of drugs to treat a disease
Interfere with the growth of microbes within atibiotics Inhibitors of Protein Synthesis
• Chloramphenicol • Broad spectrum • Binds 50S subunit, inhibits peptide bond formation
• Aminoglycosides • Streptomycin, neomycin, gentamycin • Broad spectrum • Changes shape of 30S subunit
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B • Topical • Combined with bacitracin and neomycin in overthe-counter preparation
• 1940 – Howard Florey and Ernst Chain performed first clinical trials of penicillin.
Figure 20.1
Table 20.1
The Action of Antimicrobial Drugs
Figure 20.2
Substance produced by a microbe that, in small amounts, inhibits another microbe
• Chemotherapy • Antimicrobial drugs • Antibiotic
• Selective toxicity
The use of drugs to treat a disease
Interfere with the growth of microbes within atibiotics Inhibitors of Protein Synthesis
• Chloramphenicol • Broad spectrum • Binds 50S subunit, inhibits peptide bond formation
• Aminoglycosides • Streptomycin, neomycin, gentamycin • Broad spectrum • Changes shape of 30S subunit
Antibacterial Antibiotics Injury to the Plasma Membrane
• Polymyxin B • Topical • Combined with bacitracin and neomycin in overthe-counter preparation
• 1940 – Howard Florey and Ernst Chain performed first clinical trials of penicillin.
Figure 20.1
Table 20.1
The Action of Antimicrobial Drugs
Figure 20.2
Substance produced by a microbe that, in small amounts, inhibits another microbe
抗生素PPT课件(英文精品) Antimicrobial activity of Nigella sativa oil against multi-drug resistant
S. no 1:1 1:10 1:50
No. of antibiotics to which the strain is
resistant
1
37
24
10
2
2
30
8
-
4
3
42
14
12
4
4
-
-
-
8
5
46
12
-
8
6
-
-
-
8
7
14
8
8
3
8
32
16
9
1
Effect of N. sativa oil against strains obtained from
Mean diameters of zones of inhibition in mm around 6 mm Conc. Odfisocil sinidmispcregnated with Oil
S. no
No. of antibiotics to which the
1:1
1:10
1:50
strain is resistant
抗生素PPT课件（英文精品） Antimicrobial activity of Nigella
sativa oil against multi-drug resistant Staphylococcus aureus
obtained from clinical specimens
Effect of N. sativa oil against strains obtained from Pus
1
20
20
16
--抗微生物药物(英文PPT)Antimicrobial_1
What is an Antibiotic?
• An antibiotic is a selective poison.
• It has been chosen so that it will kill the desired bacteria, but not the cells in your body. Each different type of antibiotic affects different bacteria in different ways.
• For example, an antibiotic might inhibit a bacteria's ability to turn glucose into energy, or the bacteria's ability to construct its cell wall. Therefore the bacteria dies instead of reproducing.
• In 1928, Sir Alexander Fleming, a Scottish biologist, observed that Penicillium notatum, a common mold, had destroyed staphylococcus bacteria in culture.
Susceptibility vs. Resistance of microorganisms to Antimicrobial Agents
• Success of therapeutic outcome depends on: • Achieving concentration of ATB at the site of
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•G(+): either inducible or constitutive and are ofter plasmid mediated
(2) Change permeability of outer membrane (3) Altering their PBP
β-Lactams
Penicillin groups: penicillin ring Cephalosporin groups: cephalosporin ring Monobactams: Aztreonam Carbapenems: (1) Imipenem-Cilastatin (Tienam) (2) meropenem (Mepem)
Chapter Outline
◇ Learning objectives ◇ Antibacterial Antibiotics
• Mechanisms of action and resistance • Spectrum of coverage • Pharmacology and adverse effects
抗菌药（英文PPT）Antimicrobials
Learning Objectives
Recognize the different classes of antimicrobials and their mechanisms of action. Identify the spectrum of coverage for specific antimicrobials. Describe possible adverse effects and drug interactions caused by antimicrobials. Select appropriate antimicrobials for various pathogens.
Anaerobic:
Endospore-forming: clostridium Non-endospore-forming: Actinomycetes
GRAM-NEGATIVE
Aerobic cocci: Neisseria-- N. gonorrhoeae, N.
meningitidis; Moraxella
★ ★
★ ★ ★
β-Lactams
Binding to penicillin-binding-protein (PBP) inner cell membrane endogeneous bacterial autolysis Activity depend on: (1) PBP type (2) degree of affinity to a particular PBP
β-Lactams : Penicillins
Penicillin G-like drugs:
Penicillin G/ Penicillin V
Penicillinase-resistant penicillins:
Dicloxacillin / Oxacillin / Methicillin / Nafcillin
Micrococcaceae family aureus: S. aureus non-aureus: S. epidermis
GRAM-POSITIVE RODS
Aerobic:
Endospore-forming: Bacillus Regular, non-endospore-forming: Listeria Irregular, non-endospore-forming: Corynebacterium
GRAM-POSITIVE COCCI
Micrococcaceae family M. luteus, M. roseus, and M. varians.
α-hemolysis: S. pyogenes β-hemolysis: S. agalactiae γ-hemolysis: Enterococcus / non-Enterococcus S. pneumoniae
Ampicillin-like drugs (Amino-PCNs)
Ampicillin / Ampicillin + sulbactam (Unasyn) A; clavulanic acid (Augmentin)
◇ Antifungal Drugs ◇ Antiviral Drugs ◇ Summary ◇ Review Questions
Pharmacology
Basctericidal / bacteriostatic Mode of action: concentration-dependent / time-dependent killing effect Minimal inhibitory concentration (MIC) Postantibiotic effect (PAE) Syngery / Indifference / Antogonism
Anaerobic cocci: Vellionella Rods:
(1) Enterobacteriaceae: Escherichia coli, Shigella, Salmonella, Klebsiella, Enterobacter, Proteus… (2) Pleomorphic: Haemophilus, Legionella, Pasteurella, Brucella (3) Miscellaneous: Vibrio, Campylobacter, Helicobacter (4) Nonfermenters: Pseudomonas, Acinebacter, Flavobacterium
β-Lactams
Resistance:
(1)β-Lactamase enzyme:
• nosocomial G (-) organisms: encoded on bacterial chromosomes, plasmid mediated, or carried on transposons
(2) Change permeability of outer membrane (3) Altering their PBP
β-Lactams
Penicillin groups: penicillin ring Cephalosporin groups: cephalosporin ring Monobactams: Aztreonam Carbapenems: (1) Imipenem-Cilastatin (Tienam) (2) meropenem (Mepem)
Chapter Outline
◇ Learning objectives ◇ Antibacterial Antibiotics
• Mechanisms of action and resistance • Spectrum of coverage • Pharmacology and adverse effects
抗菌药（英文PPT）Antimicrobials
Learning Objectives
Recognize the different classes of antimicrobials and their mechanisms of action. Identify the spectrum of coverage for specific antimicrobials. Describe possible adverse effects and drug interactions caused by antimicrobials. Select appropriate antimicrobials for various pathogens.
Anaerobic:
Endospore-forming: clostridium Non-endospore-forming: Actinomycetes
GRAM-NEGATIVE
Aerobic cocci: Neisseria-- N. gonorrhoeae, N.
meningitidis; Moraxella
★ ★
★ ★ ★
β-Lactams
Binding to penicillin-binding-protein (PBP) inner cell membrane endogeneous bacterial autolysis Activity depend on: (1) PBP type (2) degree of affinity to a particular PBP
β-Lactams : Penicillins
Penicillin G-like drugs:
Penicillin G/ Penicillin V
Penicillinase-resistant penicillins:
Dicloxacillin / Oxacillin / Methicillin / Nafcillin
Micrococcaceae family aureus: S. aureus non-aureus: S. epidermis
GRAM-POSITIVE RODS
Aerobic:
Endospore-forming: Bacillus Regular, non-endospore-forming: Listeria Irregular, non-endospore-forming: Corynebacterium
GRAM-POSITIVE COCCI
Micrococcaceae family M. luteus, M. roseus, and M. varians.
α-hemolysis: S. pyogenes β-hemolysis: S. agalactiae γ-hemolysis: Enterococcus / non-Enterococcus S. pneumoniae
Ampicillin-like drugs (Amino-PCNs)
Ampicillin / Ampicillin + sulbactam (Unasyn) A; clavulanic acid (Augmentin)
◇ Antifungal Drugs ◇ Antiviral Drugs ◇ Summary ◇ Review Questions
Pharmacology
Basctericidal / bacteriostatic Mode of action: concentration-dependent / time-dependent killing effect Minimal inhibitory concentration (MIC) Postantibiotic effect (PAE) Syngery / Indifference / Antogonism
Anaerobic cocci: Vellionella Rods:
(1) Enterobacteriaceae: Escherichia coli, Shigella, Salmonella, Klebsiella, Enterobacter, Proteus… (2) Pleomorphic: Haemophilus, Legionella, Pasteurella, Brucella (3) Miscellaneous: Vibrio, Campylobacter, Helicobacter (4) Nonfermenters: Pseudomonas, Acinebacter, Flavobacterium
β-Lactams
Resistance:
(1)β-Lactamase enzyme:
• nosocomial G (-) organisms: encoded on bacterial chromosomes, plasmid mediated, or carried on transposons