Introduction
s
opportunistic of weakened immune
infections
only pathogenic system
: in case
o
Psendomonas
aeruginosa
L
omnipresent grows very easy
3
,
Ly for antibiotics
resistant
many
Biofilms
3 =
layer of
microorgamisms on an surface with bacteria that cluster together
Qurorum with factors
sensing if
density wirmience
o
sensing more bacteria are present high release
=
,
Artibgiotics
s
Bacterial ribosomes have 505
llarge and 305 Isman subuemit
)
)
L 609
different than
eurariotes -3
and 405
3
Protein
synthesis
o
good target for
ribosomes
drugs
7 50
mappens at the
J Goram bacteria
-
o
thim
imner and outer membrame and
pertidoglycan layer in between
s Gramt Bacteria
o
one membrane
tnick outside
peptidloglycan layer
o
on
3
bacteriostatic inhibits division not kill bacteria needs immune
but does good system
= -3
s bactericidal :
kills the bacteria
s GP penicilling macrolides sulfa
antib o cs
Eetracyclins trimethoprim co metronidazol
:
's,
,
,
-trimoxazol,
,
,
s
Hospital antibiotics Cepmalosporins quinolomes aminoglycosides
:
,
,
resistance
3 Transfer of resistance can occur wia
:
?
o
bacterial transformation -3 release of DNUA
o
bacterial transauction phages
)
horizontal transfer
gene
-
s
bacterial plasmia DNA
conjugation
o -
s
inactivation enhanced efflux
change of
target Erug
,
.
, Biosymtnesis & struc ture
formed from amino acids 7
iso 3 V -
antibiotic -
G
3 3 penicillin penicil in pericilling
7
-APA
s
Benicillin E
acylase
PGA
Beptidoglycan crosslinking
s
:
gramn
o
-
in
directly between the u amino pepticle chains
w
gram
+
L via
pentaglyaine -3
glycine briage
3
peptidage p ro t e i n
made by trans G penicillin binding
o
)
=PBP
U
recognizes Daa
-
B
-lactam's
innibit PBP
crosslinking
3
5 no
o
's
SAR & properties
B
-NMRTEISIR.
5
membered ring
""
!
aoor
B ring
-lactaur
s
Pericillin O
o
for bacteria
only gramt
Narrow spectrumn Brosed spectrum
for fast
dividing bacteria
o
only
In oral B B B
-lactarmanse
-lactamase
-lactarmase
o
unstable at acidic conditions Penicillim Bemiciblin resistant sensitive resistamt
G V ( armoxicillin ammoxicillint clawulanicacian
flukloxacillin
allergic reactions
o
o
sensitive for B Gramt + t t t t
-lastamases
t
Gramni
t
low acid cue to
stability
3
:
wB tension and unstable
ring
-lactam
no resomance possible of amide
o
AcuI side
o
-chain
s can be improved
by
:
oadd electron withdrawing s
adsorption but for
group more
polar 50
poorer better
gram
-
.
s
ammoxicillin nas
very good bioavailability
B
-lactamases
catalyse ring opening
s
mechanism
:
L inactivates anribiotica
3
3
can cause resistance
s
sensitivity influenced byy
:
o
add steric hindrance
Lactamase innibitors inhibit lactamasesi antibacterial
activity
s no on their own
o
clavulanic acid -
suicide innibitor
s
o
salbactam
o
tazobactarn
s
opportunistic of weakened immune
infections
only pathogenic system
: in case
o
Psendomonas
aeruginosa
L
omnipresent grows very easy
3
,
Ly for antibiotics
resistant
many
Biofilms
3 =
layer of
microorgamisms on an surface with bacteria that cluster together
Qurorum with factors
sensing if
density wirmience
o
sensing more bacteria are present high release
=
,
Artibgiotics
s
Bacterial ribosomes have 505
llarge and 305 Isman subuemit
)
)
L 609
different than
eurariotes -3
and 405
3
Protein
synthesis
o
good target for
ribosomes
drugs
7 50
mappens at the
J Goram bacteria
-
o
thim
imner and outer membrame and
pertidoglycan layer in between
s Gramt Bacteria
o
one membrane
tnick outside
peptidloglycan layer
o
on
3
bacteriostatic inhibits division not kill bacteria needs immune
but does good system
= -3
s bactericidal :
kills the bacteria
s GP penicilling macrolides sulfa
antib o cs
Eetracyclins trimethoprim co metronidazol
:
's,
,
,
-trimoxazol,
,
,
s
Hospital antibiotics Cepmalosporins quinolomes aminoglycosides
:
,
,
resistance
3 Transfer of resistance can occur wia
:
?
o
bacterial transformation -3 release of DNUA
o
bacterial transauction phages
)
horizontal transfer
gene
-
s
bacterial plasmia DNA
conjugation
o -
s
inactivation enhanced efflux
change of
target Erug
,
.
, Biosymtnesis & struc ture
formed from amino acids 7
iso 3 V -
antibiotic -
G
3 3 penicillin penicil in pericilling
7
-APA
s
Benicillin E
acylase
PGA
Beptidoglycan crosslinking
s
:
gramn
o
-
in
directly between the u amino pepticle chains
w
gram
+
L via
pentaglyaine -3
glycine briage
3
peptidage p ro t e i n
made by trans G penicillin binding
o
)
=PBP
U
recognizes Daa
-
B
-lactam's
innibit PBP
crosslinking
3
5 no
o
's
SAR & properties
B
-NMRTEISIR.
5
membered ring
""
!
aoor
B ring
-lactaur
s
Pericillin O
o
for bacteria
only gramt
Narrow spectrumn Brosed spectrum
for fast
dividing bacteria
o
only
In oral B B B
-lactarmanse
-lactamase
-lactarmase
o
unstable at acidic conditions Penicillim Bemiciblin resistant sensitive resistamt
G V ( armoxicillin ammoxicillint clawulanicacian
flukloxacillin
allergic reactions
o
o
sensitive for B Gramt + t t t t
-lastamases
t
Gramni
t
low acid cue to
stability
3
:
wB tension and unstable
ring
-lactam
no resomance possible of amide
o
AcuI side
o
-chain
s can be improved
by
:
oadd electron withdrawing s
adsorption but for
group more
polar 50
poorer better
gram
-
.
s
ammoxicillin nas
very good bioavailability
B
-lactamases
catalyse ring opening
s
mechanism
:
L inactivates anribiotica
3
3
can cause resistance
s
sensitivity influenced byy
:
o
add steric hindrance
Lactamase innibitors inhibit lactamasesi antibacterial
activity
s no on their own
o
clavulanic acid -
suicide innibitor
s
o
salbactam
o
tazobactarn
