Microsoft Word - antibiotics-052.doc
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- かずまさ さんきち
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1 β β β 1
2 !"#$%&'()* 2;/0%,#FG% /0%, "-%,.% :9% #.-% 12-%,9%!"#$% +"# +"#% <=,#/0%,#DE% ".% 56% 34 78%!"#$% 2
3 β 3
4 4
5 !-Lactam Aminoglycoside Penicillin G Kanamycin A 5
6 β 6
7 7
8 andidaasperugillus 8
9 9
10 23456Growth urve7 &'# / 0 % 1 $ %!"# $%# () # *+,+ -+. treptomyces 10
11 ------cillin (Methicillin) ef (ephaloridine) treptmyces -----mycin Kanamycin Micromonospora -----micin Gentamicin 11
12 minimum inhibitory concentrationmi µ 12
13 β β 13
14 14
15 15
16 16
17 β 17
18 β ub MI + PAE post antibiotic sub MI effect (PAME) 18
19 19
20 6 p β!!"#$%&'()*+, penam cephem monobactam penem cepham oxapenam oxacephem carbapenam carbacephem 20
21 Penicillin G ( 2 ) ephalosporin 2 ( 2 ) ephamycin 21
22 β 22
23 3 3 Penicillin G Penicillin acylase Aminopenicillanic acid (6-APA) Acylation 3 R 3 emi-synthetic Penicillin 23
24 !"#$%&'( 3 3 Methicillin Ampicillin 3 3 arbenicillin Talampicillin 3 3 β 24
25 β!"#$%&'()*+ 2 ( 2 ) ephalosporin Aminocephalosporanic acid (7-AA) 2 R 3 R 1 R 2 emi-synthetic ephalosporin 25
26 β 2 + e faloridine!"#$ 26
27 2 2 efotiam!"#$ 2 2 ( 3 ) 2 2 ( 3 ) 2 + eftazidime!"#$ 2 3 a + efsulodin!"#$ Latamoxef!"#$%&'( 27
28 !"#$%&'()*+,-./ methoxy R 1 R oxime A A R 1 R 2 7-AA 2 R 3 B 2 aminothiazole 3 -methyltetrazoylthio emi-synthetic ephalosporin ( 3 ) carboxyl (sufonic) A & B 345!6789:;<=>?@AB0,D E45F7G0I=>?@JIK,D L45MP=QQAB β β 28
29 !"#$%& Thienamycin ( treptomyces cattleya ) 2 2 = 2 ( 2 ) Imipenem ilastatin Betamipron Panipenem!"#$%& ( 2 ) 2 2 ( 3 ) ulfazecin ( Pseudomonas )
30 Aztreonam arumonam!-!"#$%&'() lavulanic acid ulbactam 2 2 Ampicillin 3 3 ultamicillin ulbactam
31 β treptomycesbacillusmicromonosporaaccharopolyspola 31
32 !"#$%&'()* 6 R 1 1 R R 1 treptidine treptamine Deoxystreptamine R1 -=(2) -2-2 R2!"#$%&'()*+,-./01 6" 4" 5" 2" 1" 2 6 3" 3-D-Glucosamine D-Glucosamine 2' 4' 3' 1' 6' 4 5' Deoxystreptamine Kanamycin A 2 =( 2 ) treptidine ( 2 )= 4 5 4' 3 1' 2' 5' 3' L-treptose 1" 5" 6" 3" 2" 4" 3 -Methyl-L-glucosamine treptomycin 32
33 33
34 !"#$%&'(Kanamycin A )*+ 2 3-D-Glucosamine 2 6-D-Glucosamine 2 P 3' 2 Deoxystreptamine 34
35 2 6-D-Glucosamine D-Glucosamine Deoxystreptamine 4' P D-Glucosamine 2 6-D-Glucosamine 6' 3 2 Deoxystreptamine 4" 2 3" 6" 5" 2" 1" ' ' 2 3' 5' 4' 6' 2 Dibekacin (DKB) 6" 4" 5" 2" 1" 2 6 3" () 1 1' ' 2 4' 3' 6' 5' 2 L-(-)-g-amino- a-hydroxybutyric acid Amikacin (BB-K8) 35
36 treptomyces!"#$%&'()*+, D B A R 1 R 2 R 3 R 4 2 ( 3 ) 2 R1 R2 R3 R 4 xytetracycline Tetracycline Demethylchlortetracycline Doxycycline Minocycline 3 3 l 3 ( 3)2 36
37 !"#$%&'()*+, x 2()2 -enzyme R 1 R 2 R 3 R4 ( 3 ) Tetracyclines 37
38 14!" ( 3 ) Erythromycin
39 16!" ( 3 ) 2 3 R R 1 3 R treptomyces, Micromonospora 1 Leucomycin!"#$%&'()*+(,- 2 3oA 4 x oa oa oa R
40 40
41 treptomyces orientalis vancosamine glucose l l Vancomycin 41
42 (hloramphenicol) p l 2 D-(-)- threo -1-p -nitrophenyl-2-dichloroacetamido-1,3-propanediol R 2 R 2 l 2 l 2!"#$%&'()* L-erythro L-threo 2 D- erythro D- threo treptomyces venezuelae 42
43 !"#$%&'()*+,-./ l 2 hloramphenicol hloramphenicol acetyltransferase l l 2 hloramphenicol acetyltransferase l
44 treptomyces lincolnensis l 3 Lincomycin lindamycin Bacteroides 44
45 treptomyces fradiae 3 P 2-3 P 3 Fosfomycin Phosphoenolpyruvic acid Rifampicinp 223 Rifamycin V Rifampicin "Ansa" aphthalenoid Benzonoid 45
46 Rifampicin 2 3-Formylrifamycin V 46
47 2 2 R 2!"#$%& ulfamine ulfoneamide p-aminobenzoic acid ulfamethoxazole Trimethoprim 47
48 !"#$%&'$( Pyridine!-pyridone "-pyridone )*+$ Quinoline Quinolone 48
49 !"#$ 2 5 al idixic acid 3!%#$ 2 5 Pipemidic acid!&#$ 2 5 orfloxacin 6 F 49
50 !"#$%& Ethambutol (EB) 2 2 p-aminosalicic acid (PA) Isoniazid (I) 50
51 p Mycosamine Amphotericin B Mycosamine ystatin 51
52 λmax nm treptomyces 52
53 !"#$%&'() l 2 2 l l l Miconazole 2 2 F F Fluconazole 53
54 D p
55 55
56 56
57 Aciclovir Vidarabine Amantadine Rimantadine 3 2 n !"#$% 3 zanamivir hydrate oseltamivir phosphate 57
58 Zidovudine Didanosine ( 3 ) 3 Indinavir 58
59 p 229 biological alkylating agents 5-FU 59
60 3 p 263 Actinomycin D p 263 DA deoxyguanosine intercalate RA polymerase ar = 2 2 X 2 2 Y L-Me-Val ar L-Me-Val ar 3 Z L-Pro D-Val L-Pro D-Val X Y Z Miitomycin A : 3 3 B: 3 3 : 2 3 L-Thr L-Thr Actinomycin D Doxorubicin Mitomycin p 264 treptomyces caespitosus ( 60
61 DA DA Anthracycline rubicin : Daunomycin Daunorubicin Adriamycin Doxorubicin Aclacinomycin A Aclarubicin Doxorubicin DA intercalate DA RA DA polymerace Daunomycin Adriamycin Aclacinomycin Adriamycin 4' 4'-epi-Adriamycin 1/2 Bleomycin p 264 treptomyces verticillus 61
62 DA DA DA BleomycinBleoA2 70% B2 30% PepleomycinPeplomycin : Peplo R 2 Bleomycin A 2: R = 222( 3)2!"# $%&#'()*+,-./ ( 3)Ph 2 2 eocarzinostatin Endiine 62
63 DA eocarzinostatin!"#$%&' p 275 p 275 iclosporin (cyclosporin A) T interleukin-2 TDM 63
64 TacrolimusFK-506 ciclosporin iclosporin (yclosporin) Tacrolimus (FK-506) 64
Microsoft Word - 化学構造式集 doc
抗生物質 (Antibiotics.) (1) 複素環式のもの (eterocyclic) - ノボビオシン (ovobiocin) - セファロスポリン類 (ephalosporins) セファロスポリン核を有するもの :R1 R2 が変わる (Those which have cephalosporin nucleus: R1 and R2 to change.) R 1 R 2 -- セファロスポリン
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