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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)

-


:


Sulfonamides and Antibacterial Synergists


1932Domagk

Gerhard Domagk

1939 Nobel prize


1


2-1

  • 1.1945


2-2

  • 2.2050


3

  • ()(SD)()(SMZ)(TMP)






Wood-Fields

:,,,,,.



Synthesis of SMZ


Synthesis of TMP


Quinolone Antimicrobial and Oxazolidone Antibacterial Agents






1.; ; ; .

2.:.

3.: CNS(GABA)(Ca).


DNAIVDNA

DNAABAgyrABgyrBDNADNAADNA,DNA,BATP,,A.








Reference..2000104276-278


1

72000HPLC


2

34


3

2mol/L50h69%III


3

,50.05mol/L901%50000Lux12h



Tuberculostatics


  • 11/10





1

19441948++N-


G-

N N N;

: : (OH ) (OH)


2.




SAR

1561719- OH

2

3

48N


Synthetic antifungal agents



  • ---

  • ---


---

---

---

---


B Amphotericin B

12~37

4~7


B Amphotericin B

DMFpH410



  • 2060


1.

2.1NAr

3.Ar



1.

  • 1969


,


2.


Clotrimazole

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

Chlorophenyl)-1-imidazolidinylmethane.

Mp.140~145


Synthesis of Clotrimazole


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



Nonazloe antifungal agents

1.


  • 2.


5-B

  • 3. 5-


  • 4.Amorolfine


  • 5. Ciclopirox)

1 1


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


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