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175
Anti-infective
Agents
(f) 8-hydroxyquinoline Derivatives
Diiodohydroxyquin (iodoquinol)
Clioquinol
(g) Miscellaneous
Nitazoxanide
Metronidazole
Structure:
N
N
N
+
O
O
-
HO
Chemical name: 2-(2-Methyl-5-nitro-1H-imidazol-1-yl)-ethanol
Uses: It is used to treat a wide variety of protozoal and bacterial infections.
Side effects: Dizziness, headache, stomach upset, nausea, vomiting.
Formulations: Tablet, Syrup, Infusion and Injection.
Brand names: Flagyl, Flagyl ER, Metro.
Tinidazole
Structure:
N
N
H
N
+
O
O
-
S
O
O
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A Textbook of Pharmaceutical
Chemistry
Chemical name: 1-(2-ethylsulfonylethyl)-2-methyl-5-nitro-imidazole
Uses: It is useful in infections from amoebae, giardia, and trichomonas.
Side effects: Dizziness, headache, nausea, vomiting.
Formulations: Tablet and Syrup.
Brand names: Fasigyn, Simplotan, Tindamax.
Secnidazole
Structure:
HO
N
N
N
+
O
-
O
Chemical name: 1-(2-Methyl-5-nitro-1H-imidazol-1-yl)-propan-2-ol
Uses: It is effective as an anti-infective in the treatment of amoebiasis.
Side effects: Dizziness, headache, nausea, vomiting.
Formulations: Tablet and Syrup.
Brand names: Flagentyl, Sindose, Secnil, Solosec.
Benzimidazole
Structure:
O
N
H
N
N
N
+
O
O
-
Chemical name: N-benzyl-2-(2-nitro-1H-imidazol-1-yl)-acetamide
Uses: Benzimidazole is an antiparasitic used in the treatment of Chagas disease. Chagas
disease, also known as American trypanosomiasis, is a tropical parasitic disease caused by
Trypanosoma cruzi.
177
Anti-infective
Agents
Side effects: Fever, muscle pain, loss of appetite and trouble sleeping.
Formulations: Tablet and Syrup.
Brand names: Rochagan, Radanil.
Ornidazole
Structure:
HO
N
N
N
+
O
-
O
Cl
Chemical name: 1-Chloro-3-(2-methyl-5-nitro-1H-imidazol-1-yl)-propan-2-ol
Uses: Ornidazole is an antibiotic used to treat some protozoan infections. It has also been
investigated for use in Crohn's disease (Inflammation of bowel).
Side effects: Dizziness, headache, nausea, vomiting.
Formulations: Tablet and Syrup.
Brand name: Xynor.
Diloxanide
Structure:
O
OO
NO
ClCl
Chemical name: 4-[(Dichloroacetyl-methyl)-amino)-phenyl furan-2-carboxylate.
Uses: Diloxanide is used to treat ameba infections and luminal amebic infection.
Side effects: Flatulence, vomiting and itchiness.
Formulations: Tablet and Syrup.
Brand names: Furamide, Entamizol (In combination with metronidazole).
178
A Textbook of Pharmaceutical
Chemistry
Clefamide
Structure:
O
N
O
O
N
OH
Cl
Cl
O
Chemical name: 2,3-Dichloro-N-(2-hydroxyethyl)-N-[[4-(4-nitrophenoxy)-phenyl]-methyl]
Uses: It is an antiprotozoal agent used to treat amebiasis.
Formulation: Tablet.
Brand name: Mebinol.
Chloroquine
Structure:
NHN
N
Cl
Chemical name: (RS)-N’-(7-chloroquinolin-4-yl)-N,N-diethyl-pentane-1,4-diamine
Uses: In the treatment of amebiasis that is occurring outside the intestine.
Side effects: Muscle damage, seizures.
Formulations: Tablet, Syrup, Suspension.
Brand name: Aralen.
179
Anti-infective
Agents
Emetine
It is a plant alkaloid extracted from the ipecac root or ipecacuanha plant.
Structure:
N
O
O
H
H
H
NH
O
O
Chemical name: (2S, 3R, 11bS)-2-{[(1R)-6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolin-1-
yl]-methyl}-3-ethyl-9, 10-dimethoxy-2,3,4,6,7,11b-hexahydro-1H-pyrido[2, 1-a]-isoquinoline
Uses: It is mainly used as both an antiprotozoal and to induce vomiting.
Formulation: Injection.
Brand name: Ipecine.
Diiodohydroxyquin
Structure:
N
OH
I
I
Chemical name: 5, 7-Diiodoquinolin-8-ol
Uses: It is a primary agent used in the treatment of intestinal amebiasis in asymptomatic
carriers (cyst passers) of Entamoeba histolytica. It is also used as a secondary agent in the
treatment of balantidiasis caused by Balantidium coli.
180
A Textbook of Pharmaceutical
Chemistry
Formulations: Tablet and Suspension.
Brand names: Diodoquin, Diquinol, Amebaquin, Metodine (In combination with
metronidazole).
Clioquinol (iodochlorhydroxyquin)
Structure:
N
OH
I
Cl
Chemical name: 5-Chloro-7-iodo-quinolin-8-ol
Uses: It is an antiprotozoal and antifungal drug.
Side effects: Neurotoxicity and optic toxicity.
Formulations: Tablet and Cream.
Brand names: Enteroquinol, Dermoquinol, Dequinol.
Nitazoxanide
Structure:
O
O
O
N
N
S
N
O
O
H
Chemical name: [2-[(5-Nitro-1,3-thiazol-2-yl)-carbamoyl]-phenyl]-ethanoate.
Uses: It is a broad-spectrum antiparasitic and broad-spectrum antiviral drug that is used in
the treatment of various helminthic, protozoal, and viral infections. It is very effective as a first-
line treatment for infection caused by Blastocystis species. It is also useful in the treatment of
giardiasis and amebiasis.
Formulation: Suspension.
Brand names: Alinia, Nizonide.
181
Anti-infective
Agents
Approved New Drugs
Antiasthmatic Agents
Mepolizumab (Nucala)
Mechanism of action: It binds to IL-5 and therefore stops IL-5 from binding to its receptor
on the surface of eosinophils. It is advantageous in a severe asthma attacks.
Anti-bacterial UTI Agents
Ceftazidime-avibactam (Avycaz)
Mechanism of action: It is a combination of the cephalosporin class of antibiotic and the β-
lactamase enzyme inhibitor. It is recommended infections caused by resistant micro-organisms.
Ilumya (Tildrakizumab-asmn)
Mechanism of action: It selectively binds to the p19 subunit of IL-23 and inhibits its
interaction with the IL-23 receptor. IL-23 is a naturally occurring cytokine that is involved in
inflammatory and immune responses.
Primarily it is used for the treatment of plaque psoriasis.
Delafloxacin (Baxdela)
Mechanism of action: It inhibits the activity of bacterial DNA topoisomerase-IV and DNA
gyrase enzyme. It is mostly used for the treatment of acute bacterial skin and skin structure
infections.
Secnidazole (Solosec)
Mechanism of action: It enters the bacterial cell as a prodrug without an antimicrobial
activity. The drug is converted to an active form via the reduction of nitro groups to radical anions
by bacterial enzymes. The radical anions are thought to interfere with bacterial DNA synthesis.
It is used for the treatment of bacterial vaginosis.
Vabomere (Meropenem and Vaborbactam)
Mechanism of action: Meropenem inhibits the cell wall synthesis and Vaborbactam
potentiates the activity of meropenem against meropenem-resistant organisms. Mainly used for
the treatment of urinary tract infection.
Antiarthritis Agents
Kevzara (Sarilumab)
Mechanism of action: It is a human recombinant IgG1 antibody that binds to both forms of
interleukin 6 receptors (IL-6R). It is used in the treatment of active rheumatoid arthritis.
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A Textbook of Pharmaceutical
Chemistry
Duzallo (Lesinurad and Allopurinol)
Mechanism of action: It reduces serum uric acid levels by inhibiting the function of
transporter proteins involved in uric acid reabsorption in the kidney.
Allopurinol acts on purine catabolism, without disrupting the biosynthesis of purines. It is
used in the treatment of hyperuricemia associated with gout.
General Information
183
Chapter
Antibiotics
Antibiotics are the agents used in the prevention and cure of bacterial infections. They are
also referred to as antibacterial agents. They may either inhibit the growth of bacteria or kill the
bacteria.
Antibiotics that prevent the growth of bacteria are called bacteriostatic and which kill the
bacteria are called bactericidal. Antibiotics are considered life-saving drugs.
Antiseptics are the agents which kill the bacteria present on living cells.
Disinfectants are the agents which kill the bacteria present on inanimate objects (non-living).
Antibiotics do not fight infections caused by viruses as listed below, but they are used in
such conditions to prevent or cure the secondary infections caused by bacteria. During viral
infections, the natural immune system is compromised and hence may lead to secondary
infections.
Colds
Flu
Most coughs and bronchitis
Sore throats, unless caused by streptococci
Depending upon clinical effectiveness, a spectrum of activity, and degree of selectivity,
those inhibiting only one group of microorganisms are called narrow-spectrum antibiotics.
E.g., Bacitracin.
Antibiotics that act against both gram-positive and gram-negative bacteria are called
broadspectrum antibiotics.
E.g., Tetracyclines, Chloramphenicol, Ciprofloxacin, etc.
14
184
A Textbook of Pharmaceutical
Chemistry
Antibiotics are classified based on their sources:
(a) Natural antibiotics: These antibiotics are obtained from the large-scale fermentation
process from bacteria or fungi. E.g., Bacitracin, Polymixin, Penicillin, Streptomycin,
Tetracyclines, etc.
(b) Semisynthetic antibiotics: Natural antibiotics are derivatized through synthetic
chemistry or by altering the fermentation medium. E.g., during the commercial
production of benzylpenicillin, phenylacetic acid is added to the medium to achieve
predominance of the product.
(c) Synthetic antibiotics: The class includes antibiotics which are having a purely synthetic
origin. E.g., Chloramphenicol, ciprofloxacin, sulfonamides, etc.
Antibiotics are also classified based on their mechanism of action.
(i) Drugs that interfere with the biosynthesis of the bacterial cell walls.
E.g., Penicillins, Cycloserine, Cephalosporins, etc.
(ii) Drugs that inhibit protein biosynthesis.
E.g., Erythromycin, Lincomycin, Tetracyclines, and Chloramphenicol.
(iii) Drugs that interfere with nucleic acid biosynthesis.
E.g., Doxorubicin, Norfloxacin, Ciprofloxacin.
14.1 SULFONAMIDES
Modern chemotherapy and the concept of prodrug were successfully utilized with the
introduction of sulfonamides. They were the first effective chemotherapeutic agents to be
employed systemically.
Paul Ehrlich is regarded as the father of modern chemotherapy due to his work in this field.
He synthesized and used Atoxyl in the treatment of sleeping sickness.
NH
2
As
O
H
O
ONa
The next major achievement in the field of chemotherapy is credited to DomagK, a research
director of Bayer laboratories, who in 1932, recognized the antibacterial activity of Prontosil. It
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