ANTIMICROBIALS THAT INHIBIT THE SYNTHESIS OF CELL WALL

Beta lactam (beta lactam ring) Prevents the cross-linkage of NAM subunits
 Penicillin by binding to the enzyme that cross-link NAM
 Cephalosporin subunits
 Carbapenems
Penicillin G creates semisynthetic derivatives
More stable in acidic environment of
 Methicillin stomach, readily absorbed in the intestinal
 Imipenem tract, less susceptible to deactivation by
bacterial enzymes and more active
Vancomycin Obtained from Amycolatopsis orientalis
Cycloserine Semisynthetic; disrupt cell wall by interfering
with particular alanine-alanine bridges that
link the NAM subunits in G+ bacteria.
 Those with these bridges are
resistant to these drugs
Bacitracin Blocks the transport of NAG and NAM from
the cytoplasm out to the cell wall
MYCOBACTERIUM Disrupt the formation of this extra layer
Isoniazid (INH) (ARABINOGALACTAN-MYCOLIC) in
ethambutol mycobacterium
ANTIFUNGAL
Echinocandins Inhibit the enzyme that synthesizes glucan,
 Caspofungin without these fungal cells cannot make cell
walls
ANTIMICROBIALS THAT INHIBITS THE SYNTHESIS OF PROTEINS
Aminoglycosides Changes the shape of 30s subunit, making it
 Streptomycin impossible for the ribosome to read the
 Gentamicin codons of mRNA to read correctly
Tetracyclines Block the tRNA docking site, which prevents
the incorporation of additional amino acids
Chloramphenicol Block the enzymatic site of the 50s, prevents
translation, blocks the formation of peptide
bonds
Lincosamides Bind to different portion of the 50s,
Streptogramins preventing movement of the ribosome form
Macrolides one codon to the next; translation is frozen
and protein synthesis is halted
Mupirocin Selectively binds to the bacterial tRNA that
carries the amino acid isoleucine. Binding
prevents the incorporation of Ilu into
polypeptides. Is prescribe in topical creams
Antisense nucleic acids Block ribosomal subunits from attaching to
that mRNA with no effect on human rna
Oxazolidinones Work to stop protein synthesis by blocking
initiation of translation
ANTIMICROBIALS THAT DIRSRUPT THE CYTOPLASMIC MEMBRANES
Gramicidin Disrupt cytoplasmic membrane of targeted
cell by forming a channel through the
membrane, damaging its integrity
Polyenes (antifungal) Attach to ergosterol, a lipid constituent of
 nystatin fungal membranes, disrupting the membrane
 Amphotericin B and causing cell lysis
Azoles act by inhibiting the synthesis of ergosterol;
 Fluconazole without ergosterol, the cell’s membrane does
Allylamines not remain intact, and the fungal cell dies`
 Terbinafine
Polymyxin Produced by bacillus polymyxia. Effective
 against G-, especially against pseudomonas,
but is toxic to human kidneys. Used against
external pathogens that are resistant to other
antibacterial drugs
Pyrazinamide Disrupts transport across the cytoplasmic
membrane of mycobacterium tuberculosis.
Effective against intracellular, nonreplicating
bacterial cells
Praziquantel antiparasitic drugs, changes the permeability
Ivermectin of cell membranes of several types of
parasitic worms.
ANTIMICROBIAL TTHAT INHIBITS METABOLIC PATHWAYS
Atovaquone Interferes with electron transport in protozoa
and fungi
Heavy metals Inactivate enzyme; agents that disrupt
tubulin polymerization and glucose uptake by
many protozoa and parasitic worms; drugs
that clock the activation of viruses
Sulfanilamide/ sulfonamides Metabolic antagonist, first commercially
available antimicrobial agent.

 Structural analogs and are very

similar to PABA’s
 They compete with PABA in the active
site of the enzyme involved in the
production of dihydrofolic acid.
 The end result with competition to
PABA is the cessation of cellular
metabolism
trimethoprim Interferes with nucleic acid synthesis. It binds
to the enzyme involved in the conversion of
dihyrofolic acid to THF
Amantadine (prevent infection by influenza A) Antiviral drugs that neutralize the acid of
Rimantadine phagolysosomes and prevent viral uncoating.
Protease inhibitors Interferes with the action of protease. Used
as cocktail of drugs including reverse
transcriptase inhibitors have revolutionized
treatment of AIDS patients in industrialized
countries.
INHIBITION OF NUCLEIC ACID SYNTHESIS
Actinomycin Binds with DNA and effectively blocks DNA
synthesis and RNA transcription not only in
pathogens but in their hosts as well
Quinolones (synthetic drug) Active against prokaryotic DNA. These inhibit
Fluoroquinones DNA gyrase – enzyme necessary for correct
coiling and uncoiling of replicating bacterial
DNA. Does have a little effect on eurkaryotes
or viruses
Nucleotide2 analogs or nucleoside analogs Antimicrobials that interfere with the
function of nucleic acids.

The structures of certain nucleotide or

nucleoside analogs, such as the anti-AIDS
drug AZT, enable them to be incorporated
into the DNA or RNA of pathogens, where
they distort the shapes of the nucleic acid
molecules and prevent further replication,
transcription, or translation.
 They are also used against viruses
Rifampin Bind more readily to prokaryotic RNA
polymerase than to eukaryotic RNA
polymerase. Is more toxic to prokaryotes.
Used against M.tuberculosis and other
pathogens that metabolize slowly and thus
less susceptible to antimicrobials targeting
active metabolic processes
Clofazimine Binds to the DNA of mycobacterium leprae
and prevents normal replication and
transcription. Used to treat tuberculosis and
other mycobacterial infections
Pentamidine Bind to protozoan DNA, inhibiting the
Propamidine isethionate pathogen reproduction and development
Reverse transcriptase inhibitors part of AIDS cocktails, act against reverse
transcriptase, which is an enzyme HIV uses
early in its replication cycle to make DNA
copies of its RNA genome (reverse
transcription). Since people lack reverse
transcriptase, the inhibitor does not harm
patient