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安徽中医学院药物化学 - 制药工程教研室 PowerPoint PPT Presentation


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第 十 七 章 合成抗菌药 ( Synthetic Antibacterial Agents ). 安徽中医学院药物化学 - 制药工程教研室. 合成抗菌药的种类 :. 第一节、磺胺类抗菌药物及抗菌增效剂. Sulfonamides and Antibacterial Synergists. 1932 年 Domagk 等研究发现了 含有磺酰氨基团的 偶氮染料 百浪多息 对感染了链球菌的小白鼠有保护 作用,同时也成功地挽救了女儿的生命。由此合成 并开发出了一系列的磺胺药物。. 一、磺胺类抗菌药的发现与发展. Gerhard Domagk

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安徽中医学院药物化学 - 制药工程教研室

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Synthetic Antibacterial Agents)

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Sulfonamides and Antibacterial Synergists


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1932Domagk

Gerhard Domagk

1939 Nobel prize


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1


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2-1

  • 1.1945


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2-2

  • 2.2050


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3

  • ()(SD)()(SMZ)(TMP)


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Wood-Fields

:,,,,,.


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Synthesis of SMZ


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Synthesis of TMP


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Quinolone Antimicrobial and Oxazolidone Antibacterial Agents


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1.; ; ; .

2.:.

3.: CNS(GABA)(Ca).


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DNAIVDNA

DNAABAgyrABgyrBDNADNAADNA,DNA,BATP,,A.


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Reference..2000104276-278


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1

72000HPLC


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2

34


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3

2mol/L50h69%III


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3

,50.05mol/L901%50000Lux12h


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Tuberculostatics


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  • 11/10


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1

19441948++N-


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G-

N N N;

: : (OH ) (OH)


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2.


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SAR

1561719- OH

2

3

48N


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Synthetic antifungal agents


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  • ---

  • ---


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---

---

---

---


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B Amphotericin B

12~37

4~7


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B Amphotericin B

DMFpH410


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  • 2060


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1.

2.1NAr

3.Ar


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1.

  • 1969


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,


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2.


Clotrimazole

Clotrimazole

-(2-)-1-Diphenyl-(2-

Chlorophenyl)-1-imidazolidinylmethane.

Mp.140~145


Synthesis of clotrimazole

Synthesis of Clotrimazole


Fluconazole

Fluconazole

2-(2,4-)-1,3-(1H-1,2,4--1-)-2-2-

(2,4-difluorophenyl)-1,3-bis-(1H-1,2,4-triazol-1-yl)-propan-2-ol.

mp.137~141 .


Preparation of fluconazole

Preparation of Fluconazole


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Nonazloe antifungal agents

Nonazloe antifungal agents

1.


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  • 2.


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5-B

  • 3. 5-


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  • 4.Amorolfine


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  • 5. Ciclopirox)

1 1


Terbinafine

Terbinafine

(E)-N-(6,6--2--4-)-N--1-

(E)-N-(6,6-dimethyl-hept-2-en-4-ynyl)-N-methyl-

naphthalen-1-ylmethyl-amine,

mp.195~198 .


Synthesis of terbinafine

Synthesis of Terbinafine


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