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Monobactum
1. MONOBACTAMS
Dr. Shilpa Sudhakar Harak
Asst. Prof., Pharm. Chem.,
GES Sir Dr. M. S. Gosavi College of Pharmaceutical Education and Research, Nashik
2. Sulfazecin
First isolated useful monobactam antibiotics from
saprophytic soil bacteria
Weakly active as an antibacterial agent
Highly resistant to β-lactamases.
SAR studies eventually led to the development of
aztreonam
3. Sulfazecin
SAR studies eventually led to the development of aztreonam
3-methoxy group - responsible for β-lactamase stability in the
series,
contributed to the low antibacterial potency & poor chemical
stability of these antibiotics.
4-methyl group –
increases stability to β-lactamases and
increases activity against Gram-negative bacteria
potency against Gram-positive bacteria decreases.
4,4-Gem-dimethyl substitution –
slight decrease in antibacterial potency after oral
administration.
4. Aztreonam
Monocyclic β-lactam antibiotic
Natural molecules served as the inspiration for the synthesis
Totally synthetic parenteral antibiotic
Exclusively active towards gram-negative microorganisms,
Inactivates some β-lactamases.
MOA similar to that of the penicillins, cephalosporins, and
carbapenems,
Has strong affinity for PBP-3, producing filamentous cells as a
consequence.
5. Aztreonam
Structure Similarity:
The C3 sulfamic acid moiety attached to the β-lactam ring similar to
ceftazidime.
The sulfur at N1 is similar to C-2 carboxyl group of β-lactam antibiotics to
confuse the PBPs.
The strongly EW group - sulfamic acid group makes the β-lactam bond more
vulnerable to hydrolysis.
The monobactams demonstrate that a fused ring is not essential for
antibiotic activity.
The α-oriented methyl group at C-2 is associated with the stability of
aztreonam toward β-lactamases.
7. Tigemonam
Newer monobactam that is orally active.
It is highly resistant to β-lactamases.
The antibacterial spectrum of activity resembles that of aztreonam.
It is very active against the Enterobacteriaceae, including E. coli,
Klebsiella, Proteus, Citrobacter, Serratia and Enterobacter spp.
It also exhibits good potency against H. influenzae and N.
gonorrhoeae.
Tigemonam is not active against Gram-positive or anaerobic bacteria
and is inactive against P. aerugi
The oral absorption of tigemonam is excellent.
It could become a valuable agent for the oral treatment of UTI and
other non–life-threatening infections caused by beta-lactamase–
producing Gram-negative bacteria.