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Classification of Anti‐Bacterial Agents and Their Functions

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 Chapter 1

Classification of Anti‐Bacterial Agents and Their

Functions

Hamid Ullah and Saqib Ali

Additional information is available at the end of the chapter

http://dx.doi.org/10.5772/intechopen.68695

Abstract

Bacteria that cause bacterial infections and disease are called pathogenic bacteria. They
cause diseases and infections when they get into the body and begin to reproduce and
crowd out healthy bacteria or to grow into tissues that are normally sterile. To cure infec‐
tious diseases, researchers discovered antibacterial agents, which are considered to be the
most promising chemotherapeutic agents. Keeping in mind the resistance phenomenon
developing against antibacterial agents, new drugs are frequently entering into the mar‐
ket along with the existing drugs. In this chapter, we discussed a revised classification and
function of the antibacterial agent based on a literature survey. The antibacterial agents
can be classified into five major groups, i.e. type of action, source, spectrum of activity,
chemical structure, and function.

Keywords: anti‐bacterial agents, classification, functions

1. Introduction

Bacteria are simple one‐celled organism, which were first identified in the 1670s by van
Leeuwenhoek. Latter in the nineteenth century, concepts have been developed that there is
the strongest correlation between bacteria and diseases. Such considerations attracted interest
of the researchers not only to answer some mysterious questions about infectious diseases,
but also to find a substance that could kill, inhibit, or at least slow down the growth of such
disease‐causing bacteria. These efforts led to the revolutionary discovery of the antibacterial
agent “penicillin” in 1928 from Penicillium notatum by Sir Alexander Fleming. The discovery
unlocked the field of microbial natural products and so new agents were continually added,
such as newly introduced daptomycin, tigecycline, linezolid, and so on. Gradually, due to vari‐
ous issues arising during the use of antibacterial agents, such as the resistance phenomenon,

© 2017 The Author(s). Licensee InTech. This chapter is distributed under the terms of the Creative Commons
Attribution License (http://creativecommons.org/licenses/by/3.0), which permits unrestricted use,
distribution, and reproduction in any medium, provided the original work is properly cited.
2 Antibacterial Agents

an enormous increase in the number and types (e.g., structurally different and agent with a
slightly different pattern of activity) of the newly added antibacterial agents has been observed,
which made it necessary to review and compile the existing classification and functions of
almost all the antibacterial agents. It is aimed that this approach will be equally helpful for
researchers, clinicians, and academicians.

2. Classification

Infectious diseases are the major causes of human sickness and death. To overcome such health
care issues, antibiotics proved to be promising agents ever since they were introduced in the
1940s. Antibacterials, which are a subclass of antibiotics, have been classified earlier in several
ways; however, to make it more easily understandable, we can classify antibacterial agents into
five groups: type of action, source, spectrum of activity, chemical structure, and function [1].

2.1. Classification based on type of action

Generally, antibacterials can be classified on the basis of type of action: bacteriostatic and
bactericidal. Antibacterials, which destroy bacteria by targeting the cell wall or cell membrane
of the bacteria, are termed bactericidal and those that slow or inhibit the growth of bacteria
are referred to as bacteriostatic. Actually, the inhibition phenomenon of bacteriostatic agents
involves inhibition of protein synthesis or some bacterial metabolic pathways. As bacterio‐
static agents just prevent the growth of the pathogenic bacteria, sometimes it is difficult to
mark a clear boundary between bacteriostatic and bactericidal, especially when high concen‐
trations of some bacteriostatic agents are used then they may work as bactericidal [2]. Some
prominent examples of bacteriostatic and bactericidal antibacterials along with their mode of
action are presented in Table 1.

A. Bacteriostatic antibacterials Function

Sulphonamides They act to inhibit folate synthesis at initial stages

Amphenicols, e.g. chloroamphenicol Amphenicols work as protein synthesis inhibitors

Spectinomycin It binds to the 30S ribosomal subunit, thereby interrupting

protein synthesis
Trimethoprim It disturbs the tetrahydrofolate synthesis pathway

Tigecycline; it belongs to the glycylcycline class It is a protein synthesis inhibitor. It binds reversibly to the
30S bacterial ribosomal subunit, which blocks the binding of
amino‐acyl‐tRNA to the acceptor site on the mRNA complex.
This prohibits the incorporation of amino acids to the
developing peptide chain, thereby inhibiting protein synthesis.

Erythromycin, clarithromucin and azithromycin are They work as inhibitors of protein synthesis
macrolides

Linezolid is a member of the oxazolidinone class

Doxycycline, tetracycline, and minocycline belong to

tetracyclines class
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B. Bactericidal antibacterials Function

Penicillins, e.g. pen V, penicillin G, procaine

penicillin G, benzathine penicillin G, methicillin,
oxacillin, cloxacillin, dicloxacillin and flucloxacillin.
They belong to β‐lactams antibiotic class

Carbapenems like imipenem, meropenem, They work by interfering the synthesis of the bacterial cell
aztreonam, ticaracillinclvulnate and piperaciin‐ wall
tazobactam; these are β‐lactam/β‐lactamase
inhibitors. Some other β‐lactam inhibitors are
cephalosporin, e.g. cefotaxime, ceftriaxone,
ceftazidime, and cefepime

Gentamicin, tobramycin, and amikacin are They inhibit protein synthesis

aminoglycosides

Quinolones and flouroquinolones, such as These block bacterial DNA replication

levofloxacin, ciprofloxacin, and oxifloxacin

Vancomycine is a glycopeptide These inhibit cell wall synthesis

Polymyxin B and colistin are polymyxins These antibacterial disrupt cell membrane

Table 1. List of some bacteriostatic and bactericiadal antibacterials.

2.2. Classification based on source of antibacterial agents

Antibacterials are the subclass of antibiotics, which can be naturally obtained from fungal
sources, semi‐synthetic members which are chemically altered natural product and or syn‐
thetic. Cephalosporins, cefamycins, benzylpenicillin, and gentamicin are well‐known exam‐
ples of natural antibiotics/antibacterials. Natural antibiotics/antibacterials often exhibit high
toxicity than synthetic antibacterials. Ampicillin and amikacin are semi‐synthetic antibiotics,
which were developed to show low toxicity and increase effectiveness. Synthetic antibiot‐
ics are also designed to have even greater effectiveness and less toxicity and, thus, have an
advantage over the natural antibiotics that the bacteria are not exposed to the compounds
until they are released. Moxifloxacin and norfloxacin are promising synthetic antibiotics [3].

2.3. Classification based on spectrum of activity

This is another way of classification of antibiotics or antibacterial agents, which is based on

their target specification. In this category, the antibacterials may be either narrow or broad
spectrum. The terms narrow spectrum and broad spectrum have been interpreted not spe‐
cifically since their use in antibiotic history, but recently these acquired clear meanings in
academic and industrial fields [4, 5]. The narrow spectrum antibacterials are considered to be
those which can work on a narrow range of microorganisms, that is, they act against Gram‐
positive only or Gram‐negative only bacteria. Unlike narrow spectrum antibacterial, the broad
spectrum antibacterial affects a wide range of pathogenic bacteria, including both Gram‐posi‐
tive and Gram‐negative bacteria. Usually, the narrow spectrum antibacterials are considered
ideal antibacterials and are preferred over the broad‐spectrum antibacterials. The reason is
4 Antibacterial Agents

that the narrow‐spectrum antibiotics do not kill as many of the normal microorganisms in the
body as the broad‐spectrum antibiotics and thus has less ability to cause superinfection. Also,
the narrow‐spectrum antibiotic will cause less resistance of the bacteria as it will deal with
only specific bacteria.

Based on the spectrum of activity, both of these groups have a large and diverse library of
antibacterials. Table 2 shows all the well‐known examples of these categories.

2.4. Classification based on chemical structure

Different skeleton‐containing antibiotics display different therapeutic behaviour; therefore, it

is an ultimate need to classify antibacterials on the basis of their chemical structure. This clas‐
sification is also very important as similar structural units have similar patterns of toxicity,
effectiveness, and other related properties. Usually on a structural basis, antibacterials have

Broad‐spectrum antibacterials (examples) Narrow‐spectrum antibacterials (examples)

Ampicillin and its derivative amoxicillin are broad‐spectrum β‐Lactamase‐sensitive, first generation
antibacterials. Amoxicillin/clavulanic acid (common name co‐ include penicillin G, benzathine penicillin G,
amoxiclav) is an antibiotic useful for the treatment of a number of penicillin V, procaine penicillin, propicillin,
bacterial infections pheneticillin, azidocillin, clometocillin, and
penamecillin are considered in narrow‐
spectrum antibacterial category

Quinolones [6] such as Maxaquin (lomefloxacin), Floxin (ofloxacin), β‐Lactamase‐resistant, Ist generation include;
Noroxin (norfloxacin), Tequin (gatifloxacin), Cipro (ciprofloxacin),
Avelox (moxifloxacin), Levaquin (levofloxacin), Factive Cloxacillin (dicloxacillin flucloxacillin),
(gemifloxacin), Cinobac (cinoxacin), NegGram (nalidixic acid), Trovan methicillin, nafcillin, oxacillin and temocillin
(trovafloxacin), and Zagam (sparfloxacin) are considered as broad‐ are narrow‐spectrum antibacterials
spectrum antibacterials

Aminoglycosides which are broad‐spectrum antibacterials Cephalosporins (first generation and second
include kanamycin A, amikacin, tobramycin, dibekacin, generation) antibacterials are relatively
gentamicin, sisomicin, netilmicin, neomycins B, C and neomycin E narrow spectrum
(paromomycin) [7]

Cephalosporins (third, fourth, and fifth generations) are relatively Vancomycin, clindamycin, isoniazid, rifampin,
extended to the broad spectrum of activity ethambutol, pyrazinamide, bacitracin,
polymixins, sulfonamides, glycopeptide and
Carbepenems (e.g. imipenems) show a broad pattern of activity [8] nitroimidazoles are counted in this group

Macrolides such as erythromycin, roxithromycin, clarithromycin,

azithromycin, and dirithromycin are considered in this category [9]

Tetracycline, chlortetracycline, oxytetracycline, demeclocycline,

lymecycline, meclocycline, methacycline, minocycline, and
tigecycline are considered as broad‐spectrum antibacterials

Chloramphenicol

Ticarcillin, a carboxypenicillin, also has a broad spectrum of activity

Rifamycins also exhibited broad coverage [10]

Table 2. List of broad‐ and narrow‐spectrum antibacterials.

 Classification of Anti‐Bacterial Agents and Their Functions 5
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been classified into two groups: group A (β‐lactams) and group B (aminoglycosides). However,
in a more elaborated way, the antibacterials can be classified into β‐lactams, β‐lactam/β‐lacta‐
mase inhibitor combinations, aminglycoside, macrolides, quinolones, and flouroquinolones.

2.4.1. β‐Lactams

Beta‐lactams are a popular class of drugs, having a four‐membered lactam ring (Figure 1),
known as β‐lactam ring; however, they vary by side chain attached or additional cycles.
Penicillin derivatives, cephalosporins, monobactams, and carbepenems, e.g. imipenems, all
belong to this class.
Usually, alterations were made to the basic penam and cephem structural units such that
enhanced antimicrobial potential is achieved. Among such modified agents, some are cla‐
vulanate, latamoxef, loracarbef, etc. On the cephalosporins unit, most changes have been
made at positions 7 and 3. Cephalothin, cephaloridine, and cephazolin are among some of
the modified cephalosporins, which have shown good activity against Gram positive with
the exception of enterococci‐ and methicillin‐resistant staphylococci. Some other examples
include preparation of microbiologically active oxacephems and carbacephems (Figure 2) by
modification of the cephalosporin nucleus [11].

The aminopenicillins are also included in this class, which are structural analogues of ampicil‐
lin, which is a 2‐amino derivative of benzylpenicillin [12].

2.4.2. Aminglycoside

In compounds of this group, two aminosugars joined by glycosidic bond to an aminocyclitol. Com-
monly used aminoglycosides are streptomycin, gentamicin, sisiomicin, netilmicin, kanamycin,

Figure 1. Basic structure of the β‐lactam ring, penicillins (Penam skeleton) and cephalosporins (Cephem skeleton). R in
Penam and Cephem nucleus represents the side chain that could be different for different penicillins and cephalosporins,
while R′ denotes another side chain in the Cephem nucleus.

Figure 2. Cephalosporin‐modified structure of oxacephems and carbacephems.

6 Antibacterial Agents

amikacin, neomycin, tobramycin, toframycin, spectinolycin, and paromonucin. The structure of

some of these is presented in Figure 3.

Changes in original structural units of aminoglycosides can be made either synthetically or

enzymatically. Structural properties such as the number and location of various functional
groups on a modified compound compared to their parent compounds usually exhibit great
effect on the biological activities of these drugs. The literature [13] has shown that the number
and location of amino groups on the hexoses and the site of attachment of the other rings to
deoxystreptamine have a considerable effect on preventing inhibition of protein synthesis or,
in other words, their biological activities. For example, among kanamycin A, B, and C, kana‐
mycin B is a highly effective antibiotic than either kanamycin A or C. It is inferred that the
presence of a diamino hexose results in a compound that has better efficiency for inhibition of
protein synthesis than the one holding only one amino group.

2.4.3. Macrolides

Macrolides belong to the polyketide class of natural products. Structurally, macrolides are
antibiotics that consist of a macrocyclic lactone ring, usually 14‐, 15‐, or 16‐member to which
one or more deoxy sugars, usually cladinose and desosamine, may be attached. Some well‐
known examples of macrolides are erythromycin and roxithromycin etc.
So far, the relationship of structural activity of various macrolides has been studied. Studies
revealed that some existing 14‐, 15‐, and 16‐member macrolide antibiotics were modified
toward interesting targets. For example, specific substitution on the C‐9, C‐11, C‐12, or C‐6
sites in the macrolactone ring results in better in vitro activity against mycobacterium tuber‐
culosis (Figure 4) [14].

2.4.4. Quinolones and flouroquinolones

Quinolones are quinine‐derived structural units and have been proved to be potent synthetic
antibacterial agents. The basic skeleton of the quinolone molecule is presented in Figure 5. The
addition of flourine at position 6 is called flouroquinolone. In the bicyclic ring, the variation

Figure 3. Structures of some well‐known aminoglycosides antibacterials.

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Figure 4. Substitution effect on activity of macrolides.

Figure 5. Basic structure of quinolone.

at positions 1‐, 5‐, 6‐, 7‐, and 8‐ exerts key effect on the therapeutic behaviour of these drugs.
Usually, such structural alteration has led to enhanced coverage and potency of antibacte‐
rial activity and pharmacokinetics, e.g. improved anti‐Gram‐positive activity of moxifloxacin
and garenoxacin. However, some of these modifications are associated with definite adverse
effects [15]. Some well‐known examples of quinolone include nalidixic acid (first generation),
ciprofloxacin (second generation), levofloxacin (third generation), and trovafloxacin (fourth
generation).

2.4.5. Streptogramin antibiotics

Streptogramin antibiotics are a unique class of antibacterials consisting of two groups of

structurally unrelated molecules: group A streptogramins (polyunsaturated macrolactones)
and group B streptogramins (cyclic hexadepsipeptides) [16]. Dalfopristin and quinopristin
8 Antibacterial Agents

are representative example of the streptogramin A and streptogramin B groups, respectively.

Alteration of the group B structural units has been mainly achieved on the 3‐hydroxypico‐
linoyl, the 4‐dimethylaminophenylalanine, and the 4‐oxo pipecolinic residues. Modifications
on this third part result in water‐soluble derivative quinupristin. Water‐soluble group
A derivatives were obtained by some synthetic steps, e.g. dalfopristin, which is a sulfone
derivative that can be obtained by Michael addition of aminothiols to the dehydroproline
ring of pristinamycin IIA, followed by oxidation [17]. The group A molecules impede with
the expansion of the polypeptide chain by avoiding the binding of aminoacetyl‐tRNA to
the ribosome and the creation of peptide bonds, while the group B building blocks encour‐
age the disconnection of the peptidyl‐tRNA and can interfere with the removal of the com‐
pleted polypeptide by blocking its access to the channel through which it usually leaves the
ribosome.

2.4.6. Sulphonamides

Sulphonamides are one of the important class of synthetic organic compounds with great
medicinal importance having a sulphonamide functional group (R1‐SO2‐NR2R3) in their struc‐
tures. Some compounds belonging to this group also show antibacterial properties such as
sulfadiazine. The original antibacterial sulphonamides are synthetic antimicrobial agents that
contain the sulphonamide group. Some others are sulfonylureas and thiazide diuretics which
proved to be newer drug groups based on the antibacterial sulphonamides (Figure 6).

2.4.7. Tetracyclines

Tetracyclines are four rings hydrocarbon containing compounds, which can be defined
also as “a subclass of polyketides having an octahydrotetracene‐2‐carboxamide skeleton.”
These antimicrobial agents were originally derived from Streptomyces bacteria, but the
newer derivatives are semi‐synthetic. Some promising examples of this group are oxytetra‐
cycline and doxycycline.

2.4.8. Nitroimidazoles

Nitroimidazoles are a group of compounds that contain a basic imidazole ring. The most com‐
monly used example is metronidazole (Figure 7). Nitroimidazoles vary by the location of the
nitro functional group. Most of the drugs of this class have their nitro group at position 6, such
as metronidazole, and/or at position 2, such as benznidazole.

Figure 6. Basic structural unit of sulphonamide.

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Figure 7. Structure of metronidazole.

2.5. Function‐based classification of antibacterial drugs

Function means how a drug works or what is its mode of action. This is one of the most impor‐
tant factors related to each antibacterial. The major processes or functions, which are responsible
for bacterial growth, are cell wall synthesis, cell membrane function, protein synthesis, nucleic
acid synthesis, and so on. All such processes are targets for antibiotics; therefore, antibacterials,
which interfere or disturb these processes in different ways, can be subdivided into four groups:
such as cell wall synthesis inhibitors, inhibitors of membrane function, inhibitors of protein syn‐
thesis, and inhibitors of nucleic acid synthesis. All these groups are discussed briefly hereafter.

2.5.1. Cell wall synthesis inhibitors

Structurally, the bacterial cell wall is different from that of all other organisms by the presence
of polysaccharide backbone, called peptidoglycan, which is composed of alternating N‐ace‐
tylmuramic acid and N‐acetylglucosamine residues in equal amounts and most of eubacteria
have peptidoglycan‐based cell walls except the mammalian cell. Like all other organisms,
the bacterial cell wall offers structural completion to the cell; therefore, the most important
process for avoiding bacterial growth is to stop cell wall synthesis by inhibiting the peptido‐
glycan layer of bacterial cell walls. The agents used to work against this function are called
cell wall synthesis inhibitors and the cell wall of new bacteria growing in the presence of these
agents is deprived of peptidoglycan.
β‐Lactam drugs, including penicillin derivatives, cephalosporins, monobactams, and car‐
bapenems, are the major antibiotics that inhibit bacterial cell wall synthesis. To understand the
­inhibition process, one must be aware of the fact that the last step in the synthesis of peptidogly‐
can is eased by penicillin‐binding proteins; therefore, this initially occurs in the binding of drug to
cell receptors, i.e. penicillin‐binding proteins. Thus, β‐lactam drugs work as a false molecule for D‐
alanyl‐D‐alanyl transpeptidases, which result in inhibition of transpeptidation reaction and pep‐
tidoglycan synthesis. Thereafter, autolytic enzyme inhibitors get inactivated, which activates the
lytic enzyme, thereby resulting in division of bacteria provided that the environment is isotonic
[18]. Some other antibiotics such as bacitracin, teicoplanin, vancomycin, ristocetin, and novobio‐
cin must be subjected at early stages, which impede early phases of the peptidoglycan synthesis.
Gram‐positive and Gram‐negative bacteria vary in the susceptibility to the β‐lactam drugs
because of the structural differences in their cell wall, i.e. Gram‐negative bacteria usually have
10 Antibacterial Agents

less susceptibility because these antibiotics fail to reach the cell wall as they are blocked by the
outer membrane of the Gram‐negative bacteria. Factors such as the amount of peptidoglycan,
receptors, and lipids availability, nature of crosslinking, autolytic enzymes activity greatly
influence the activity, permeation, and incorporation of the drugs.

Considering the resistance phenomenon, all β‐lactam antibacterials can only be inactivated
by bacterial produced enzymes called β‐lactamases (e.g. penicillinases, cephalosporinases,
cephamycinases, carbapenemases, and so on).

2.5.2. Inhibitors of membrane function

The cytoplasmic membrane, which covers the cytoplasm, serves as a selective barrier and
controls the internal composition of the cell. Whenever these functional roles of the cytoplas‐
mic membrane get disturbed, macromolecules and ions will outflow, which will result in cell
destruction or death. Selectivity of the agents is necessary to carry out this chemotherapy as
the agents are aimed to target the bacterial cell membrane. Polymyxins are active antibacte‐
rial agents, which are cyclic peptides, having a long hydrophobic tail. Polymyxins are found
in the form of A, B, C, D, E, where B and E can be used therapeutically. Polymysins show
their specificity for polysaccharide molecules, which are present in the outer membrane of
many Gram‐negative bacteria; therefore, polymyxins are considered to be selectively toxic for
Gram‐negative bacteria. Mechanistically, after association with the lipopolysaccharide sub‐
strate in the outer membrane of Gram‐negative bacteria, polymyxins change the membrane
structure so that its permeability increases, which results in disruption of the osmotic balance.
Additionally, changes like discharge of the molecules from interior of the cell, inhibition of
respiration, and increased water uptake lead to the cell death. Since Gram‐positive bacteria
have a too thick cell wall, which denies the access of these molecules to the Gram‐positive
bacterial cell membrane, polymyxins have less or even no effect on Gram‐positives [19].

2.5.3. Protein synthesis inhibitors

Protein synthesis is one of the most important functions in the bacterial cell and humans as well.
Therefore, to cure infectious disease caused by pathogenic bacteria, it is the most important tar‐
get for the drugs, which are called protein synthesis inhibitor antibiotics. Since both human and
bacterial cells synthesize proteins, due to the slow synthesis of human proteins, it has remained
a comfortable task for the development of the selective antibiotics. Only the side effects from
toxicity and resistance phenomenon are taken seriously during antibiotic development.
Mechanistically, protein synthesis inhibitors act to disturb any stage of the protein synthesis
such as initiation and elongation stages (aminoacyl tRNA entry, proofreading, peptidyl trans‐
fer, ribosomal translocation and termination). Table 3 shows representative antibiotics, their
sites and pathways, etc. [20].

2.5.4. Inhibition of nucleic acid synthesis

One of the most important targets for antibiotic to cure infectious diseases is nucleic acid
synthesis, and the antibiotics used are called nucleic acid synthesis inhibitors. A sound
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Drug type Binding site function and pathway disturbed

Aminoglycosides: Examples include Aminoglycosides bind to the 30S ribosomal subunit which alter the
gentamicin, tobramycin, streptomycin, and ribosomal structure. This affects all normal steps of protein synthesis,
kanamycin such as initiation step of translation, blocking of elongation of peptide
bond formation, discharge of incomplete, and toxic proteins. These
disturbances ultimately stop protein synthesis and destroy the
cytoplasmic membrane.

Macrolides These are protein synthesis inhibitors, which bind to the 50S ribosomal
subunits, impeding peptidyl transfer

Tetracyclines and glycyclines (tigecycline) These inhibitors bind to the 30S ribosomal subunit. Protein translation
(through inhibition of aminoacyl tRNA binding to ribosome) gets
disturbed by these inhibitors

Strptogramines: Examples include Their binding site is the 50S ribosomal subunit. They interfere in
pristinamycin, dalfopristin, and protein translation through prevention of initiation, elongation, and
quinupristin translocation stages and free tRNA depletion

Phenicols: For example, chloroamphenicol These antibiotics, e.g. chloroamphenicols, bind to the 50S ribosomal
subunit and inhibit protein synthesis by blocking the peptidyl transfer
phase of elongation on the 50S ribosomal subunit in bacteria

Oxazolidinone: The most common They bind to the 50S ribosomal subunit, which are thought to act at the
example is linezolid initiation stage [21]

Ketolides: This is a novel class of protein synthesis inhibitors, which exhibit excellent activity against resistant
organisms.

Protein synthesis inhibitors with unknown pathway include retapamulin, mupirocin, and fusidic acid.

Table 3. Example of drugs, their binding sites and pathways which get affected.

difference in the enzymes that carry out DNA and RNA synthesis between eukaryotic
and prokaryotic cells helps to achieve selective toxicity, which favours development of
the antibiotic. The antibacterials of this class can be subdivided into DNA inhibitors and
RNA inhibitors. RNA inhibitors interfere with the bacterial transcription process in which
messenger RNA transcripts of genetic material are produced for later transformation into
proteins. RNA inhibitors such as rifampin, a well‐known example of the rifamycins family,
bind to DNA‐dependent RNA polymerase, thereby creating a wall that inhibits elongation
of RNA. Such a situation prevents gene transcription which affects the normal function of
bacteria that results in cell death. Like all other biological polymerization processes, DNA
synthesis is also achieved by initiation, elongation, and termination stages; therefore, anti‐
bacterial drugs target any one of these processes to inhibit DNA synthesis. Quinolones,
including nalidixic acid and ciprofloxacin, work as DNA inhibitors. DNA gyrase (a topoi‐
somerase) is accountable for cutting one of the chromosomal DNA parts at the beginning
of the supercoiling. The scratch is made provisionally and later on linked back together.
Quinolones bind to DNA gyrase, inhibiting their function, which results in inhibition of the
DNA replication that ultimately results in cell damage. There are some other antibacterial
drugs, which act upon anaerobic bacteria by creating metabolites that are bind into DNA
strands, which then are more likely to rupture. Examples of such drugs include nitrofuran‐
toin and metronidazole.
12 Antibacterial Agents

3. Recent antimicrobial agents

Our discussion covered almost all the old and some new antimicrobial agents. However, to
make these agents easily understandable, Table 4 lists some recent antibacterial agents with
their structure, class, and so on [22].

FDA‐approved Structure Category Approval year/

antibacterial agent trial phase
Tigecycline Glycylcycline 2005

Doripenem Carbapenems 2007

Retapamulin Pleuromutillin 2007

Telavancin Glycopeptides 2009

Ceftaroline Cephalosporins 2010

Fidaxomicin Macrocyclic 2011

FDA approval awaiting Structure Category Approval year/

antibacterial agents trial phase

Ceftobiprole Cephalosporin Awaited

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FDA‐approved Structure Category Approval year/

antibacterial agent trial phase
Iclaprim Dihydropholate Awaited
reductase
inhibitor

Torizolid Oxazolidinones Phase II

Radezolid Oxazolidinones Phase II

Cethromycin Ketolides Phase III

Solithromycin Ketolides Phase II

Oritavancin Glycopeptide Phase III

14 Antibacterial Agents

FDA‐approved Structure Category Approval year/

antibacterial agent trial phase
Dalbavancin Glycopeptide Phase III

Table 4. List of newer antibacterial agent.

4. Conclusion and prospectives

Unlike antibiotics classification, little efforts have been made to classify antibacterials (a subclass
of antibiotic) separately. Therefore, we tried to classify antibacterial into five principal catego‐
ries, each of which has its own importance. However, classifications based on chemical structure
and function of these agents are considered to be more important as these groups describe a lot
about their therapeutic nature, while the rest of the classification is less important, e.g. some‐
times, classification based on the spectrum of activity distinguishes these agents in an ambig‐
uous way as the spectrum sometime depends on their concentration used. The classification
mentioned could be a better guide for future classification, i.e. the agents that are in developing
stages or those that are going to develop can be adjusted in any suitable group mentioned in the
text. Further, this categorization could be helpful in academic and in health care fields at present
and in the future as well.

Author details

Hamid Ullah1,2* and Saqib Ali2

*Address all correspondence to: [email protected]

1 Department of Chemistry, Faculty of Arts and Basic Sciences, Balochistan University of
Information Technology, Engineering and Management Sciences (BUITEMS), Quetta, Pakistan

2 Department of Chemistry, Mohi‐ud‐Din Islamic University, AJ&K, Pakistan

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