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Phn cng cng vic:

- Trn Vn Hng: Tm ni dung v lm slide


- Nguyn Vn Mnh: Tm ni dung v lm slide
- Hong Th Thanh Hng: Tm ni dung
- Nguyn Th Thu Hin: Tm ni dung
i cng v nhm Tetracylin

I.Cng thc cu to chung


V lch s, thnh vin u tin ca nhm thuc ny l Chlortetracycline
cui nhng nm 1940 do tin s Benjamin Duggar, mt nh khoa hc lm
vic cho Lederle Laboratories, ng chit sut cht ny t mt vi khun
mu vng, ging nh nm c tn l Streptomyces aureofaciens.
Oxytetracycline c khm ph trong thi gian rt ngn bi AC Finlay v
cng s, n cng ging nh trch t vi khun trong t l Streptomyces
rimosus. Robert Burns Woodward xc nh cu trc ca Oxytetracycline,
ri tng hp nn tetracycline. S pht trin ca cc khng sinh c thay i
v cu trc ha hc t nhm ny. Vo thng 6 nm 2005, tigecycline-
thnh vin u tin ca nhm mi ca tetracyclines c tn l
glycylcyclines c gii thiu iu tr nhim trng m khng vi cc
loi khng sinh khc, k c tetracyclines c in. Trong khi tigecycline l
thuc tetracycline u tin c chp nhn hn 20 nm qua, cc phin
bn mi khc ca tetracyclines hin vn ang th nghim lm sng trn

ngi.

-c im cu to.
H tetracyclic vi nhiu ni i lin hp.
Nhm OH phenol.
NHm N base.
Nhm ceton.
Nhiu C bt i
II. Lin quan c ch v tc dng

S lin kt tuyn tnh ca 4 vng l yu t quan trng nht n kh nng


hot ng ca khng sinh.

Nu thay chc OH v tr (3) bng bt k nhm chc khc th s b mt


hot tnh.

V tr lin kt i v tr 2-3 rt quan trng n kh nng hot tnh ca


khng sinh.

- Cc yu t duy tr hoc lm tng hot tnh.


Hai vng A/B cu hnh cis; h thng in t phn cch qua C12a gn OH
l bt buc duy tr hot tnh.
Nhm N(CH3)2 (4) lin kt th tetracyclin mi c hot tnh, nu epi ha
hot lc gim 90 %.
Kh nng chuyn dng thun nghch gia ng phn h bin do cng
hng vng A l yu t bo tn hot tnh.
Cc nhm th lm tng hot tnh: Cl, -NO2 (7), -OH (5).
- Cc yu t lm gim hot tnh.
Nhm th -Cl (9), -NH2(7)
Chelat gia tetracyclin vi cc kim loi a ha tr.
pH>8, vng C ca mt s tetracyclin b ph hy, nhm th -Cl (7) thc y
nhanh s phn hy ny.
III. C ch tc dng.

Tc dng km khun l do gn trn tiu phn 30s ca ribosom vi khun,


ngn cn RNAt chuyn acid amin vo v tr A trn phc hp ARNm -
riboxom to chui polypeptid

IV. Ph tc dng.
Ph rng nht.
Tc dng trn vi khun Gram (+)
- Streptococcus pyogenes
- Streptococcus viridans
- Staphylococcus pyogenes

Gram (-)
- Neisseria gonorrhoeae
- Neisseria meningitides
- Haemophillus influenza
- E.Coli ( km nhy cm
Vi khun k kh.
Vi khun gy bnh khng in hnh nh Rickettsia, Coxiella burnetii,
Mycoplasma pneumoniae
Mt s xon khun nh Borrelia recurrentis, Borrelia burgdorferi (gy bnh
Lyme), Treponema pallidum (giang mai), Treponema pertenue.
Hin nay t l khng tetracyclin ca vi khun gy bnh rt cao.

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