8- khang sinh tong hop - ct - 2011

1KHKHNG SINH TNG SINH TNG HNG HPP

2sulfamid khng khun

3Ngay t nhng nm u th k 20 cc nh khoa hc nhn thy rng cc phm nhum c tc dng khng khun , tuy nhin cc phm nhum thng rt c.

LCH S TM RA SULFAMID

Nm 1913 ngi ta tm thy phm azoic cryzoidin c tc dng dit khun v tng i t c.

NN

NH2

H2N

Azoic cryzoidin

4NN

NH2

H2N

Azoic cryzoidin

SO2NH2

Prontosil

Khi c thm nhm - SO2NH2 trong cng thc cc phm nhum thng rt bn v gn cht vo protein.

Ngi ta th gn thm vo phn t cryzoidin nhm sulfamido, v thu c mt cht c tc dng chng t cu v lin cu l prontosil


51935 Bovet v Trefuel pht hin ra rng prontosil khng c tc dng trn in vitro m ch c tc dng trn in vivo

In vitro

In vivo


6Prontosil ?

Vo c th prontosil chuyn ha thnh cht khc ctc dng khng khun


7NH2 H2NSO2 + NaNO2HCl +H

-Cl]N[NH2NSO2

NH2

H2N

SO2NH2N

NH2

H2N N

(Sulfanilamid)

m - phenylendiamin

p - aminobenzensulfonamid

Nguyn liu u tng hp protosil lp-aminobenzensulfonamid

Prontosil


8Khi thay th sulfanilamid bng amin khc cho sn phm khng c tc dng khng khun

+ NaNO2HCl

NH2

H2N

anilin

+H-Cl]N[NNH2

NN

NH2

H2N

m - phenylendiamin


9NH2 H2NSO2 + NaNO2HCl +H

-Cl]N[NH2NSO2

Sulfanilamid

OH

NN

NH2

HO

Khi thay th m - phenylendiamin bng cht khc cho sn phm c tc dng khng khun

phenol


O2SNH2

10

Bovet v Trefuel th v thy sulfanilamid c tc dng khng khun trn cin vitro v trn in vivo. Ngoi ra sn phm acetyl sulfanilamid xut hin trong nc tiu

sulfanilamid NH2 H2NSO2

CH3COOH

SO2NH2CH3CONH


11

Sulfanilamid tr thnh sulfamid u tin trong lch s. Vic pht hin ra prontosil v sulfanilamid m ra mt knguyn mi cho vic ha tr liu cc bnh nhim khun. Da trn cu trc sulfanilamid ngi ta tng hp rt nhiu sulfamid trong khong 40 loi c s dng lm thuc.


12

LIN QUAN GiA CU TRC V TC DNG DC LC

14

N lun lun phi v tr C4 ( para vi SO2NH )

R1NH

R1NH

NHR1

NHR1

SO2NHR1

SO2NHR1

R2NH

R2NH

N lun lun phi gn vi nhn thm

R2NHCH2

Sulfamylon

Thay i trn N4

13

14SO2NHR1R2NH

Thay NH2 C4 bng nhm khc u lm mt tc dng nhng nu thay bng NO2 vn cn tc dng nhng c

SO2NHRO2N


14

Thay i trn N4

N lun lun phi t do COOH

COOH NHSO2N

SHN H2N

Ftalazol

Sulfathiazol


15

Khi thay th nhn benzen bng cc nhn khc u lm gim hoc mt tc dng nhng c th to ra cc tc ng khc.

Mi s th trn nhn u lm gim hoc mt tc dng.

SO2NHR1R2NH

R

R

R

R

Thay i trn nhn thm


16

Khi thay nhm sulfamid bng cc nhm khc u lm gim hay lm mt tc dng.Khi th H bng cc nhm th mch thng ni chung lm gim tc dng tr trng hp sulfaguanidin v sulfacetamid th bng d vng cho tc dng tt.

H2N SO2NHR C

NH

NH2

Sulfaguanidin

COCH3

Sulfacetamid

N

SSulfathiazol

Th nhm sulfamid


17

iU CH SULFAMID

i t anilin

NH2 + (CH3CO)2O NHCOCH3

NH2 + HCOOH NHCOCH3

NH2 + ClCOOC2H5 NH COOC2H5

Bo v nhm amin

18

H2N H ClSO2HO ClH2N SO2+

ClH2N SO2

NH3

2RNH

CH3CO NH2SO2NH

NHRSO2NH CH3CO

clorosulfon ha

To nhm sulfamoyl nh tc dng ca NH3 hay RNH2

iU CH SULFAMID

19

CH3CO NH2SO2NH

Thy phn gii phng sulfamid

SO2NH NH2HCl.

SO2NH2H2N SO2NH2H2N

SO2H2N NHNa

HCl

HClNaOH

NaOH

iU CH SULFAMID

20

i t clorobenzen

ClHOSO2Cl

SO2Cl

ClNH3

SO2NH2

Cl NH3

80 atSO2NH2

NH2

200oC

iU CH SULFAMID

21

i t cc sulfamid c sn

H2N SO2NH2 + CH2NNH2

NH

NH2

NHNH-CH2N SO2

H2N SO2NH2 + (CH3CO)2O NHCOCH3SO2H2N

NH2

NHNH-CH2N SO2 +

HCOHC

C H2N SO2 NHN

N

Sulfanilamid

Sulfanilamid Sulfaguanidin

Sulfacetamid

Sulfaguanidin Sulfadiazin

iU CH SULFAMID

22

TNH CHT SULFAMID

NH2H2N SO2

OH

H2N

O

S=NH

ONa

S=NH

O

H2N

Cho ta mui Ag, Cu, Co

NH2H2N SO2HCl

NH2H2N SO2HCl.

Tnh cht ha hc

Tnh acid

Tnh base

23

NH2 H2NSO2 + NaNO2HCl +H

-Cl]N[NH2NSO2

SulfanilamidOH

NH2NSO2 N

Nhm amin thm cho phn ng diazo ha thng dng nh tnh v nh lng

TNH CHT SULFAMID

24

Nhn benzen cho cc phn ng th c th p dng nh tnh hay nh lng

SO2NH2

NH2

+ Br2

NH2Br Br

SO2NH2

TNH CHT SULFAMID

25

Nhm NH2 c th phn ng vi p-aminobenzaldehyd ( PDAB) cho sn phm c mu c th dng nh tnh v nh lng

+

CN=H2N H N

CH3

CH3

NH2H2NSO2 NHOCCH3

CH3

TNH CHT SULFAMID

26

nh tnh

cc phn ng musc kph hng ngoit ngoiTh tinh khitCloridSulfatGim khi lng do sy khTp cht lin quan

Rf

IR UV

KiM NGHIM SULFAMID

27

KiM NGHIM SULFAMID

nh lng

Diazo ha

NH2 H2NSO2 + NaNO2HCl +H

-Cl]N[NH2NSO2

KI + h tinh bt

Ch th ngai Ch th ni

Tropeolin OO Chun th

pp dng c

28

+

CN=H2N H N

CH3

CH3

NH2H2NSO2 NHOCCH3

CH3

Phng php quang

Mu vng

Phng php quang

KiM NGHIM SULFAMID

29

nh lng sulfamid bng phng php acid-base

NaOH 0,1NChun mi trng nc

sulfadiazin, sulfacetamid( acid mnh )

Cc sulfamid( acid yu )

Natrimethylat 0,1N

xanh thymol (CT)

dimethylformamid

Chun mi trng khan

Cc sulfamid( base yu )

HClO 4 0,1N

Tm tinh th (CT)

Acid acetic bng

Chun mi trng khan

KiM NGHIM SULFAMID

30

Phng php kt ta

NH2 H2NSO2 + AgNO 3 SO2NHH2N Ag

Cn

KiM NGHIM SULFAMID

31

iu ch:- T Anilin- T Clorobenzen.- Bn tng hp t cc sulfamid c sn

Lin quan cu trc tc dng:

- Nhn thm, nhm sulfamid (-SO2NHR), nhm amin thm t do v tr para vi -SO2NHR

- Nhm th cc v tr khc trn nhn thm lm mt tc dng.

- R: c th thay i v lm thay i tc dng iu tr, c quan ch.

32

Tnh cht:- Tnh lng tnh:

-NH2 cho tnh base;- SO2NHR cho tnh acid To mui vi KLN

- Nhm amin thm bc 1:- Phn ng diazonium- To mu vi TT PDAB

- Nhn thm: cho phn ng th vi- Khi t cc sulfamid khc nhau chy cho cn mu khc nhau

33

Kim nghim:- nh tnh- Kim tinh khit- nh lng

- PP Diazo ha- PP quang- PP kt ta- PP acid base:

- Mi trng thng- Mi trng khan

34

DC NG HC

Hp thu

Tr mt s sulfamid khng hp thu qua ng tiu ha v c s dng tr nhim khun ng rut nh ftalazon, sulfaguanidin

a s cc s sulfamid hp thu nhanh qua ng rut. Khong 70%

H2N SO2 NH

N

NNH2

NHNH-CH2N SO2

Sulfaguanidin ( khng hp thu ) Sulfadiazin (hp thu tt )

35

- Sulfamid c phn phi khp cc t bo ca c th. - Sulfamid c th nhanh chng i vo mng phi, hot

dch mt v cc dch tng t.- Kh nng thm vo mng no thay i ty thuc vo

loi sulfamid; mc gn protein; mc acetyl ha vmc tn thng ca mng no. Th d: sulfadiazin vo mng no 17% trn ngi thng nhng trn ngi b vim no c th ti 66%.

- Sulfamid thng qua c nhau thai.

Phn phiDC NG HC

36

Chuyn ha

Kh nng acetyl ha sulfamid ty thuc vo c a bnh nhn v loi sulfamid s9a vo c th

SO2NH2CH3CONHNH2 H2NSO2CH3COOH

- Cc dn cht acetyl ha ca sulfamid thng khng ctc dng, tuy nhin mt s cht gy kt tinh thn.

- Ngy nay ngi ta to ra nhng loi sulfamid t b acetyl ha hoc c dn xut acetyl ha d tan :

- sulfamethoxypiridazin c t l acetyl ha 10%

- sulfadiazin c dn cht acetyl ha tng i d tan

DC NG HC

37

Ph khng khun

Sulfamid c ph khng khun rng:

Gr (+) : t cu, lin cu, ph cu, lu cu

Gr (-) : trc khun l, thng hn, E.Coli

X khun.

Virus mt ht

TAC ONG DC LC

38

C TNH SULFAMID

c tnh trn mu- Ri lon h thng to mu do hin tng mn cm,- Hin tng tan huyt lin quan ti s hot ha glucose- 6 phosphat dehydrogenase. - Phn ng khng ph thuc vo nng sulfamid mvo tng c th v tng sc dn v thng xy ra trong tun u dng thuc.

Triu chng c th l- Bun nn, st, chng mt, vng da, xanh xao trong trng hp nng c th l thiu mu bt sn. - Tm ti do to methemoglobin.

39

c tnh trn thn

Sulfamid c th c th kt tinh thn gy tn thng thn, vim thn, si thn i ra mu.

Nhc im ny c khc phc dn do tm c nhng sulfamid t acetyl ha, t kt tinh..

Cn ch :Ung nhiu nc

Ung dung dch kimKhng dng cho tr em

C TNH SULFAMID

40

- Phn ng ny rt khc nhau i vi tng sulfamid vvi tng ngi thng hay xut hin khi dng sulfamid tc ng chm. - Triu chng: c th l ni ban , xut huyt Khi dng ngoi c th gy nm da do kch thch s nhy cm ca da vi tia t ngoi

C TNH SULFAMID

Phn ng tng nhy cm

41

MT S SULFAMID KHNG KHUN CHNH

Phn loi

Hp thu tt qua ng tiu ha v khuch tn tt ti cc t chc trong c th.

Nhm c chia ra thnh cc nhm :

Sulfamid tc ng nhanh

Sulfamid tc ng chm

Sulfamid tc ng trung gian

Sulfamid tc ng ton thn

42

Sulfamid dng ngai

t hp thu vo mu nn ch tc dng ti ch.

Nhm ny c chia ra thnh cc nhm:

Sulfamid ng rut

Sulfamid ng tiu

Sulfamid tc ng ti ch

Phn loi

MT S SULFAMID KHNG KHUN CHNH

43

SULFAMID TON THN

Sulfamid tc dng nhanhhp thu nhanh v thi tr nhanh nn phi ung nhiu ln trong ngy.t lin hp proteinThng l nhng sulfamid th h uD gy kt tinh thno thi nhanh t tch ly nn tng i t c

44

SULFANILAMID

Ch nh

- y l sulfamid u tin trong lch s trc kia c coi l thn dc v c tc dng trn mng no cu, lin cu.

- Hin nay t dng trong iu tr v c tnh tng i cao v b acetyl ha nhiu (80%).

- Ngy nay ch yu c dng lm nguyn liu tng hp sulfamid khc.

NH2 SO2H2N

45

SULFATHIAZOL

Ch nh

- Dng trong iu tr t nm 1940 v l mt trong nhng sulfamid c tc dng tt nht chng t cu, lu cu, mng no cu, ph cu.

- t c.

- D hp thu t nhanh nng cao trong mu.

- T l acetyl ha khong 30%.

H2N SO2NHS

N

46

SULFADIAZIN

Ch nh

Sulfadiazin l mt trong s t sufamid cn s dng nay.

t tan nhng hp thu nhanh v bi tit chm nhanh chng t nng cao trong mu.

Trn invitro n tc dng km sulfathiazol nhng invivo mnh hn v t c hn

N

NNHH2N SO2

47

SULFAMID TC NG CHM

- Gm nhng sulfamid hp thu nhanh vo mu nhng tn ti lu trong c th.- C kh nng lin hp vi protein ln nn thi trchm. - t b acetyl ha (10%) tin cho vic tr liu v ch cn dng mt liu duy nht trong ngy.- Cc sulfamid ny u c cha trong phn t nhm CH3O, mt nhm ny th khng cn tc dng ko di.- Cn thn vi nhng ngi nhy cm v thuc c thtich ly

48

SULFAMETHOXYPYRIDAZIN

OCH3H2N SO2NHN N

Ch nh

- Hp thu nhanh v thi tr rt chm nn ch cn ung 1g / ngy.- c tnh tng t cc sulfamid khc nhng khi ng c th c im thi tr chm li l im bt li.- Nu th H ca -SO2NH bng -CH3CO ta c acetylsulfamethoxy- pyridazin khng ng thch hp vi tr em.

49

SULFADOXIN

NN

NHH2N SO2

OCH3 OCH3

Ch nh

Thi tr rt chm ch cn dng 1g / tun.

Sulfadoxin + pyrimetamin FANSIDAR tr st rt

50

SULFAMID TC NG TRUNG GIAN

- Hp thu nhanh v tc thi tr va phi phn tn u trong c th.

- t b acetyl ha thng ung ngy 2 ln.

- Cc sulfamid nhm ny thng c d vng 5 cnh.

- Hin nay mt s sulfamid nhm ny cn s dng ph bin.

51

SULFAMETHOXAZOL

Ch nh

y l sulfamid c dng ph bin hin nay thng dng tr nhim trng ng tiu, nhim trng da.

Bactrim c th thay th cloramphenicol chng thng hn

BACTRIMSulfamethoxazol 800 mgTrimethoprim 160 mg

N O CH3

NHSO2H2N

52

SULFAMID TI CH

Sulfamid ng tiu

Ni chung c th dng nhng sulfamid trn tr nhim khun ng tiu.

Ngi ta thng chn nhng sulfamid thi tr nhanh t acetyl ha d tan.

Tuy nhin cng c nhng sulfamid chuyn dng tr nhim khun ng tiu.

Nhm mch thngNhm d vng: thng c nhm CH3 v d vng 5 cnh

53

SULFACETAMID

Ch nh- D tan trong nc hn nhiu sulfamid khc, nhanh chng t nng cao trong mu, nhng thi trnhanh, t kt tinh . - Do thi gian tc dng ngn nn t c dng lm thuc khng khun ton thn.- Thng lm thuc khng khun ng tiu v to nng cao trong nc tiu. - Cn c s dng lm thuc nh mt tr mt ht.Mui Na d tan khng gy kch ng nim mc.

NHCOCH3SO2H2N

54

Sulfamid ng ruot

Cc sulfamid nhm ny khng tan v khng hp thu qua ng tiu ha nn t nng cao rut v c s dng tr cc bnh ng rut nh t,l, vim rut. Trong s ny tr sulfaguanidin chuyn bit tr bnh ng rut, cc sulfamid khc u i t nhng sulfamid thng thng c gn thm nhng nhm chc lm cho cc cht ny khng hp thu qua ng tiu ha v tc ng ti ch.

SULFAMID TI CH

55

SULFAGUANIDIN

Ch nh

y l sulfamid dng ph bin nc ta.

Do t tan trong kim nn khng hp thu rut.

t c nn c th dng liu cao .

Tuy nhin sulfaguanidin c nh hng ti vi khun ng rut, nn ung thm men tiu ha v ung km B1

H2ONH

NH2CH2N SO2NH

56

Sulfamid dung ngoaiNi chung t s dng cc sulfamid tr nhim khun da do s c mt ca PABA trn cc vt thng v s tng mn cm ca da khi dng sulfamid.

Mt s sulfamid c s dng dng ngoi di dng thuc bt hay thuc m nh sulfanilamid, sulfadiazin.

Mui bc sulfadiazin c tc dng khng khun rt tt.

2H2N SO2NH H2N SO2N

NN

Ag

SULFAMID TI CH

57

Sulfamid dng ngoi

Ngoi cc sulfamid trn c mt sulfamid chuyn sdng ngoi da v khng chu tc ng bi PABA lsulfamilon

CH2NH2 SO2NH2

SULFAMID TI CH

58

thuc khng khun nhm quinolon

59

. I CNG NHM QUINOLON

Lch sThuc u tin: acid nalidixic (negram), mt

thuc khng khun tng hp tr nhim khun ng tiu bi vi khun Gram (-) t 1964.

60

Cc quinolon th h I

YX

NO

O COOH

O

ten thuoc X Y R

acid oxolinic H H C2H5cinoxacin N H C2H5mibxacin H H OCH3


61

X

Y N

COOH

O

R1

R2

ten thuoc X Y R1 R2acid piromidic N N C2H5

acid pipemidic N N C2H5

resoxacin H H C2H5

N

HNN

N

Cc quinolon th h I. I CNG NHM QUINOLON

62

- Cc quinolon th h 1 khng cha F (trflumequin).- Hp thu km v chuyn ha nhiu gan thnh sn phm khng c tc dng. - Ph khng khun hp , ch c tc dng trn mt s vi khun ng rut v ng tiu: E. coli, Proteus, Samonella, Enterobacter, gonorrhea. - khng nhanh do hin nay t c sdng.

Cc quinolon th h I. I CNG NHM QUINOLON

63

N

F

O

COOH

NN

R2

R3R1 R4

ten thuoc R1 R2 R3 R4Perfloxacin CH3 H H C2H5nofloxacin H H H C2H5Amifloxacin CH3 H H NHCH3ofloxacin CH3 H

Ciprofloxacin H H H

lomefloxacin H CH3 F C2H5Enoxacin H H N C2H5

OCH3

Cc quinolon th h II


64

Cc quinolon mi

OCOOHF

ON

HN

H

H H3C

Moxifloxacin ( Avelox)

F

N

H2N

N

O

COOH

F

F

Trovafloxacin

O

H3C

N N

COOH

O

F

N

NH2

Gemifloxacin


65

Lin quan cu trc v tc ng dc lc

87

65 4 3

21

N

COOHO

h thng pyridon phi ngng t vi nhn thm. - V tr 1 th alkyl ngn ( methyl, ethyl, cyclopropyl ) tng tc dng khng khun.

C2H5CH3


66

- Vic th v tr 2 lm gim hay hy tc dng.

- Vic th ng cu in t N cho C v tr 2 (cinnolin), 5 ( 1,5- naphthyridin) , 6 ( 1,6-naphthyridin), 8 (1,8- naphthyridin) vn duy tr tc dng khng khun.

87

65 4 3

21

N

COOHO

RN

NN

N


67

87

65 4 3

21

N

COOHO

V tr 3 bt buc phi l COOH

V tr 4 Nhm C=O khng c thay i

V tr 5,6 khi th lm gim tc dng

R

R

Th F v tr 6 lm tng tc dng khng khun

F


68

- V tr 7 th lm gim tc dng tr s th nhn pyperazinyl hay d vng.- Thm nhm N-CH3 lm tng thi gian bn hy- V tr 8 c th th bng F cho tc dng tt.- Vng ngng t 1-8 cho tc dng tt

87

65 4 3

21

N

COOHO

NN

H3CF

CH3O


69

Ha tnh

-Tnh bn: Cc quinolon u khng bn ngoi nh sng.

- Phn ng kt ta: Quinolon base cho phn ng kt ta vi cc thuc th chung alkaloid.

- Nhm acid c th cho phn ng to ester

- Nhm C=O cho phn ng vi Natrinitroprusiat cho mu tm.

- Phn ng to phc: Cc quinolon u c th to phc chelat vi cc ion ha tr 2,3 nh Ca2+, Mg2+, Al3+, Fe 3+ .


70

Kim nghimnh tnh.1/ Cc phn ng to ta, phc, mu. 2/ Cc phng php ha l: ph t ngoi, hng ngoi, sc k lp mng, sc k lng hiu nng cao.nh lngPhng php mi trng khan : HClO4 / CH3COOH


Tc ng dc lc- Fluoroquinolon c ph khng khun rng c bit c hiu qu cao chng vi khun Gram (-) hiu kh.- Hiu qu trong iu tr Staphylococcus aureus, nhng hin nay c s khng.

71

C ch tc ng. c ch hot tnh enzym AND gyrase , ngn cn qudui xon chui AND, c ch s sao chp AND.

T bo ngi khng cha DNA gyrase, nhng cha topoisomerase enzym c chc nng tng t.

Fluoroquinolon ch c ch DNA gyrase liu iu tr; nng cao hn gp 100- 1000 ln s c chtopoisomerase.


72

AND gyrase

Quinolon


73

Phn ng ph- Fluoroquinolon tng i t phn ng ph v t c tnh. - Ri lon tiu ha: bun nn, au bng, kh chu- Ni m ay, d ng- Ri lon th gic- Tng s mn cm da vi nh sng mt tri- Nhng bin chng v sn thy ng vt cha trng thnh khi dng liu ln hn liu cho ngi do c khuyn co nhng thuc ny khng nn dng cho tr em di 16 tui


74

Ch nh. - Tr norfloxacin, do kh nngsinh hc km khi

ung, nn ch hn ch trong iu tr nhim trng ng tiu nh cc quinolon th h 1.

- Cc quinolon cn li s dng trong nhim trng ng tiu, sinh dc, a chy, thng hn, h hp, xng, tin lit, lao


75

CIPROFLOXACIN

F

O

COOH

NHN

ten khac: cipro, ciflox

C 17H18FO3N3 p.t.l 331,35

Ten khoa hoc : acid 1-Cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolin carboxylic

76

Kim nghim.nh tnh

Ph hng ngoiSc k lp mng Phn ng ca ion FPhn ng ca C=O : vi Natri nitroprusiat cho mu tm

Th tinh khitCl-, SO42-, kim loi nng, tro sulfat

nh lngSc k lng cao p Mi trng khan

CIPROFLOXACIN

77

Tc dng dc lc- Ciprofloxacin c tc dng trn khun hiu khGram(-) gm c thng hn.- Hin xut hin s khng trn chng Pseud. aeruginosa. - Trc y c tc dng trn mt s chng Gr (+), nhng hin nay khng nhiu

CIPROFLOXACIN

Cng dng iu tr cc bnh nhim trng h hp, tai, mi, hng, thn, ph khoa, gan mt, tin lit, xng, khp, bnh rut, thng hn, l.

78

Tc dng ph- Fluoquinolon c th gy thng tn sn, cn thn cho tr em < 16 tui- Dng km corticoid c th tng nguy c phn ng ph. - Dng cn thn trn bnh nhn b cc bnh v gan, thn.- Ciprofloxacin c th gy phn ng ph h thn kinh trung ng, nh ri lon thn kinh, trm ut, hoa mt, o gic, run, kch ng, lo lng, ng g, au u, mt ng, kh chu, ri lon v m, chng mt,...

CIPROFLOXACIN

79

OFLOXACIN

N

O

COOH

O

F

NN

CH3H3C

ten khac : ofloset, Exocin; Flobacin; Floxil; Floxin; Oflocet Oflocin; Ox aldin;

C 18H20FO4N3 p.t.l 331,35

Ten khoa hoc: acid (+)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-

piperazinyl)-7-oxo-7 H- pyrido[1,2,3- d ]-1,4-benzoxazin-6-carboxylic

H1

H1 Hp, 3/19/2008

H2 Hp, 3/19/2008

80

Tc ng dc lc

- Ofloxacin c thi gian bn hy trung bnh

- C tc dng trn nhm vi khun Gr (-) nhng yu hn so vi Ciprofloxacin.

- Ofloxacin c hiu qu chng lu cu v nhim trng niu o do Chlamydia.

- Nhng nghin cu gn y cho thy ofloxacin ctrin vng trong ha tr liu ci. Hin ang nm trong chng trnh chng ci ca OMS

OFLOXACIN

81

SPARFLOXACIN

NN

HN

H3C

CH3

F

F

NH2COOH

O

Ten khac : Spara, ZagamC 19 H 22 F 2 N 4 O 3 p.t.l. 329,41acid (cis) -5-Amino-1-cyclopropyl-7-(3,5-di methyl-1-piperazinyl)-6,8-difluoro-1,4 dihydro-4-oxo-3-quinolin carboxylic

82

SPARFLOXACIN

Sparfloxacin l quinolon th h th hai. c FDA cho php 1996

Ch nh

Vim phi v nhim khun nng.

Vim ph qun mn tnh.

Vim xoang.

83

MOXIFLOXACINO

COOHF

ON

HN

H

H H3C

( Avelox)

Ch nh. Nhim trng ng h hp, nhim trng da

8- khang sinh tong hop - ct - 2011

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