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Chemistry in our life


Here we try to show the continuous researches in chemistry

Welcome 2009/09/09

thank you for joining Chemicals in medicines


me
Chemicals in medicines

Hello everybody The words ‘medicine’ and 'drug' are often used in our country to mean
the same substances: any substance, manufactured artificially, which
here you can find
can help recovery from sickness, relieve symptoms or modify a natural
what u need in
process in the body. A medicine is often a mixture of several chemical
chemistry and you
can ask any question
compounds. Even if it has only one active component compound often
other substances are used as fillers or binders to give it bulk. Chemistry,
the science related to chemical substances, provides us the tools to
Who Am I? make and study the substances that are the constituents of almost all
medicines. The past hundred years or so, ever since the advent of
organic chemistry, many chemical compounds have been discovered in
nature that are effective for curing diseases. Modern chemistry has also
made it possible to synthesize several medicines using methods of
organic chemistry
esraa hashim

i'm chemist girl The most common medicines can be classified into few groups, e.g.
View my complete antibiotics; antiseptics; analgesics; and antipyretics etc. While an
profile antibiotic is a drug that kills or prevents the growth of bacteria, an
analgesic is often used to relieve pain

Followers list There are very many medicines that come under each of these groups.
Followers (8) Often several chemical compounds that make a particular group of
medicines, say antibiotics have similar chemical structure. Since the
medicines in a particular group are effective for treating a particular type
Pages of ailment or disease, their mode of action can also be very similar. But,
the main page the methods used to isolate a medicine from its natural sources or to
synthesize it are most often very different

what's your In this project, I have tried to find out the relationships between chemical
opinion about structures of medicines in three groups of medicines, viz. Antibiotics;
this link? Antipyretics and Analgesics. I have also explored the mode of action of
these groups of medicines and the chemical methods used to make
them available

Antibiotics

Our body and our domestic animals, can serve as hosts to a wide variety
of disease-causing organisms (pathogens): These are
bacteria
viruses
fungi
protozoon’s
blog list Here we will examine only those chemicals that are used to combat
bacterial pathogens An antibiotic (Greek anti, "against"; bios, "life"), is a
chemical substance produced by one organism that is destructive to
Chemistry &
another. This process traditionally has been called antibiosis and is the
Technology
- ‫ﺣﺳﺎﺳﯾﺔ اﻟﺣﯾواﻧﺎت اﻟﻣﻧوﯾﺔ‬ opposite of symbiosis. More specifically, an antibiotic is a type of
‫ﻣﺎ ھﻰ وﻣﺎ ﺣﻠﮭﺎ؟؟‬ chemotherapeutic agent that has a toxic effect on certain types of
3 years ago disease-producing microorganisms without acting dangerously on the
patient. The definition most used for antibiotics is: any substance
produced by a microorganism which harms or kills another
science ..

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6/4/2019 Chemistry in our life: Chemicals in medicines
Chemical forums microorganism. However, antibiotics DO NOT harm viruses. Doctors
6 years ago
often prescribe antibiotics when you may have a viral infection because
of the possibility that you may also acquire a bacterial infection because
Chemistry in our you are so ill with a virus - being ill places a person at risk for certain
life bacterial infections that are normally handled without any problem
Pi-stacking better The overwhelming majority of antibiotic substances are natural products
without the that certain bacteria and fungi (molds) produce and send outside of their
aromatics?
7 years ago cells. About 90% of the antibiotics in use today, are isolated from
bacteria. There are a few antibiotics, however, which are completely
synthetic... that is, are made from scratch in the laboratory. These
Blog Archive particular antibiotics are designed to inhibit some process previously
identified to be completely unique to bacteria, and necessary for the
July (11) bacterium to remain alive
June (50) An antibiotic can be most often classified into any one of the following
May (48) categories of chemical compound
April (44) Aminoglycosides
Glycopeptides
March (53)
Beta Lactams also known as Penicillins
February (59)
Tetracycline
January (37) Quinolines
December (38) Sulfonamides
November (53) Aminoglycosides
October (57)
Aminoglycosides are antibiotics that are often administered into veins or
muscle to treat serious bacterial infections. Some aminoglycosides are
September (46)
also used orally to treat intestinal infections or topically to treat eye
August (27) infections. Some very popular examples of this group of antibiotics are
July (5) Examples are
October (11) Streptomycin
September (10) Kanamycin
Neomycin
Gentamycin

Glycopeptides
Glycopeptide antibiotics are a class of antibiotic drugs. They consist of a
glycosylated cyclic or polycyclic nonribosomal peptide. Important
glycopeptide antibiotics include vancomycin, teicoplanin, ramoplanin,
and decaplanin
This class of drugs inhibit the synthesis of cell walls in susceptible
microbes by inhibiting peptidoglycan synthesis. Due to their toxicity, their
use is restricted to those patients who are critically ill or who have a
demonstrated hypersensitivity to the β-lactams

Penicillins are one major class of antibiotics. They are used to treat
strep throat and countless other infections. Examples of various kinds of
penicillins include
Amoxicillin
Ampicillin
Azlocillin
Carbenicillin
Cloxacillin
Dicloxacillin
Flucloxacillin
Mezlocillin
Nafcillin
Penicillin
Common structural features of Beta-Lactams; (The beta-lactams get
their name from the characteristic ring structure — shown here in blue —
that they all share. (The green arrow shows the bond that is broken by a
class of enzymes called beta-lactamases that are synthesized by many
(penicillin-resistant bacteria
Tetracycline
Tetracyclines are another category of antibiotics. In addition to being
used to treat infections, they are often used to manage acne. A few of
the tetracyclines frequently used are
(Achromycin V® (Tetracycline §
(Minocin® (Minocycline §
(Vibramycin® (Doxycycline §

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6/4/2019 Chemistry in our life: Chemicals in medicines

The chemical structure of most tetracycline is related to the following


structure. One can see that the name is derived from the fact that it is
madeup of four rings (cycles
Examples of commonly used tetracycline’s include
Demeclocycline
Doxycycline
Minocycline
Oxytetracycline
Tetracycline

Quinolones
The quinolones are a family of broad-spectrum antibiotics. The parent of
the group is nalidixic acid. The majority of quinolones in clinical use
belong to the subset of fluoroquinolones, which have a fluoro group
attached the central ring system. Quinolones and fluoroquinolones are
bactericidal drugs, actively killing bacteria. Quinolones inhibit the
bacterial DNA gyrase or the topoisomerase II enzyme, thereby inhibiting
DNA replication and transcription

Sulfonamides
Sulfonamide drugs (known widely as "sulfa drugs") were the first
antibacterial antibiotics, and paved the way for the antibiotic revolution in
medicine. The first sulfonamide was trade named Prontosil, which is a
prodrug. Experiments with Prontosil began in 1932 in the laboratories of
the Bayer Corporation, a component of the huge German chemical trust
IG Farben. The dye-based drug was synthesized by Bayer chemist
Josef Klarer and tested in animals under the direction of
physician/researcher Gerhard Domagk. Domagk quickly won the 1939
Nobel Prize in Medicine and Physiology, an honor that Hitler forbade him
to accept
Some examples of sulfonamide antibiotics are
Mafenide
Prontosil
Sulfacetamide
Sulfamethizole
Sulfanilimide
Sulfasalazine
Sulfisoxazole
Trimethoprim
(Trimethoprim-Sulfamethoxazole (Co-trimoxazole) (TMP-SMX

Analgesics
Analgesics are medicines that help to control pain and reduce fever. An
analgesic (colloquially known as a painkiller) is any member of the
diverse group of drugs used to relieve pain (achieve analgesia). This
derives from Greek an-, "without", and -algia, "pain". Examples of
analgesics that are available over the counter are: aspirin,
acetaminophen, ibuprofen, ketoprofen and naproxen sodium. Some
analgesics contain a combination of ingredients in one pill, such as
aspirin, acetaminophen and caffeine
Analgesics act in various ways on the peripheral and central nervous
system; they include paracetamol (acetaminophen), the nonsteroidal
anti-inflammatory drugs (NSAIDs) such as the salicylates, narcotic drugs
such as morphine, synthetic drugs with narcotic properties such as
tramadol, and various others. Some other classes of drugs not normally
considered analgesics are used to treat neurop athic pain syndromes;
these include tricyclic antidepressants and anticonvulsants
Thus acetylsalicylic acid (commonly known as aspirin) is a salicylate

Aspirin is commercially synthesized using a two-step process. First,


phenol (generally extracted from coal tar) is treated with a sodium base
generating sodium phenoxide, which is then reacted with carbon dioxide
under high temperature and pressure to yield salicylate, which is
acidified, yielding salicylic acid. This process is known as the Kolbe-
Schmitt reaction

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Antiseptics

Antiseptics are antimicrobial substances that are applied to living


tissue/skin to to reduce the possibility of infection, sepsis, or
putrefaction. They should generally be distinguished from antibiotics that
destroy microorganisms within the body, and from disinfectants, which
destroy microorganisms found on non-living objects. Some antiseptics
are true germicides, capable of destroying microbes (bacteriocidal),
whilst others are bacteriostatic and only prevent or inhibit their growth.
Antibacterials are antiseptics that only act against bacteria
Some chemical compounds/groups of chemical substances that are
often used as antiseptics are
Alcohols
Most commonly used are ethanol (60-90%), 1-propanol (60-70%) and 2-
propanol/isopropanol (70-80%) or mixtures of these alcohols. They are
commonly reffered to as "surgical alcohol". Used to disinfect the skin
before injections are given, often along with iodine (tincture of iodine) or
some cationic surfactants (benzalkonium chloride 0.05 - 0.5%,
(chlorhexidine 0.2 - 4.0% or octenidine dihydrochloride 0.1 - 2.0%

Quaternary ammonium compounds


They include the chemicals benzalkonium chloride (BAC), cetyl
trimethylammonium bromide (CTMB), cetylpyridinium chloride (Cetrim),
cetylpyridinium chloride (CPC) and benzethonium chloride (BZT).
Benzalkonium chloride is used in some pre-operative skin disinfectants
(conc. 0.05 - 0.5%) and antiseptic towels. The antimicrobial activity of
Quats is inactivated by anionic surfactants, such as soaps. Related
disinfectants include chlorhexidine and octenidine

Boric acid
Used in suppositories to treat yeast infections of the vagina, in
eyewashes, and as an antiviral to shorten the duration of cold sore
attacks. Put into creams for burns. Also common in trace amounts in eye
contact solution. Though it is popularly known as an antiseptic, it is in
reality only a soothing fluid, and bacteria will flourish comfortably in
contact with it

Chlorhexidine Gluconate
A biguanidine derivative, used in concentrations of 0.5 - 4.0% alone or in
lower concentrations in combination with other compounds, such as
alcohols. Used as a skin antiseptic and to treat inflammation of the gums
(gingivitis). The microbicidal action is somewhat slow

Hydrogen peroxide
Used as a 6% (20Vols) solution to clean and deodorise wounds and
ulcers. More common 1% or 2% solutions of hydrogen peroxide have
been used in household first aid for scrapes, etc. However, even this
less potent form is no longer recommended for typical wound care as
the strong oxidization causes scar formation and increases healing time.
Gentle washing with mild soap and water or rinsing a scrape with sterile
saline is a better practice

Iodine
Usually used in an alcoholic solution (called tincture of iodine) or as
Lugol's iodine solution as a pre- and post-operative antiseptic. No longer
recommended to disinfect minor wounds because it induces scar tissue
formation and increases healing time. Gentle washing with mild soap
and water or rinsing a scrape with sterile saline is a better practice.
Novel iodine antiseptics containing iodopovidone/PVP-I (an iodophor,
complex of povidone, a water-soluble polymer, with triiodide anions I3-,
containing about 10% of active iodine, with the commercial name
Betadine) are far better tolerated, don't affect wound healing negativelly
and leave a depot of active iodine, creating the so-called "remanent," or
persistent, effect. The great advantage of iodine antiseptics is the widest
scope of antimicrobial activity, killing all principial pathogenes and given
enough time even spores, which are considered to be the most difficult

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form of microorganisms to be inactivated by disinfectants and antiseptics

Mercurochrome
Not recognized as safe and effective by the U.S. Food and Drug
Administration (FDA) due to concerns about its mercury content.
Another obsolete organomercury antiseptics include bis-(fenylmercury)
(monohydrogenborate (Famosept

Phenol (carbolic acid) compounds


Phenol is germicidal in strong solution, inhibitory in weaker ones. Used
as a "scrub" for pre-operative hand cleansing. Used in the form of a
powder as an antiseptic baby powder, where it is dusted onto the belly
button as it heals. Also used in mouthwashes and throat lozenges,
where it has a methadone-like painkilling effect as well as an antiseptic
one. Example: TCP. Other phenolic antiseptics include historically
important, but today rarely used (sometimes in dental surgery) thymol,
today obsolete hexachlorophene, still used triclosan and sodium 3,5-
(dibromo-4-hydroxybenzenesulfonate (Dibromol

Sodium chloride
Used as a general cleanser. Also used as an antiseptic mouthwash.
Only a weak antiseptic effect, due to hyperosmolality of the solution
above 0.9%

Sodium hypochlorite
Used in the past, diluted, neutralised and combined with potassium
permanganate in the Daquin's solution. Nowadays used only as
disinfectant

.How Antibiotics act


Antibiotics attack a metabolic pathway found in the bacterium but not in
the host. This is not an insurmountable problem for bacterial pathogens
.because they differ in many respects from eukaryotes
Thus pencillins (beta-lactams) work by interfering with the synthesis of
the bacterial cell wall — a structure that is not found in eukaryotes. The
walls of bacteria are made of a complex polymeric material called
peptidoglycan. It contains both amino acids and amino sugars. The
amino sugars are of two kinds
N-acetylglucosamine (NAG) and its close relative
.(N-acetylmuramic acid (NAM
These two form a linear polymer of NAG alternating with NAM. They are
linked by a glycosidic bond between the #1 and #4 carbons (this is the
linkage attacked by lysozyme) and are oriented in the same way they
are in cellulose. Side chains containing 4 or 5 amino acids are attached
to each NAM. These form covalent bonds with amino acids in adjacent
chains. The bonds may
be direct to the next chain or
include additional peptide cross bridges (e.g., 5 glycine residues)
which
extend to chains in the same plane (shown here) as well as to
chains above and below
This elaborate, covalently cross-linked structure provides the great
strength of the cell wall. It also leads to the remarkable conclusion that
!the bacterial cell wall meets the definition of a single molecule
The beta-lactam antibiotics bind to and inhibit enzymes needed for the
synthesis of the peptidoglycan wall. While they have little effect on
resting bacteria, they are lethal to dividing bacteria as defective walls
cannot protect the organism form bursting in hypotonic surroundings

The aminoglycosides bind to the 30S subunit of the bacterial ribosome,


because the bacterial ribosome differs in several ways from the
eukaryotic ribosome and thus interferes with the formation of the
initiation complex , causing misreading of the mRNA

Tetracyclines also bind to the 30S subunit of the bacterial ribosome.


They prevent the transfer of activated amino acids to the ribosome so

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protein synthesis is halted

The fluoroquinolones block the action of two bacterial topoisomerases


— enzymes that relieve the coils that form in DNA when the helix is
being opened in preparation for replication or transcription or repair

The mode of action of Sulfonamides is a bit different. Both bacteria and


their human hosts require folic acid for nucleic acid synthesis (it is
converted into prunes and thymidine) as well as protein synthesis
(precursor of the amino acids methionine and glycine). However,
bacteria synthesize their folic acid starting with para-aminobenzoic acid
(PABA), while we must ingest our folic acid already formed; that is, for us
.it is a vitamin
Sulfanilamide, and the other sulfa drugs, are analogs of PABA; they
compete with PABA and, when chosen, block the synthesis of folic acid.
Mammals ignore PABA and its analogs and thus can tolerate sulfa drugs

Production of antibiotics

Since the first pioneering efforts of Florey and Chain in 1939, the
importance of antibiotics to medicine has led to much research into
discovering and producing them. The process of production usually
involves screening of wide ranges of microorganisms, testing and
modification. Production is carried out using fermentation; a process that
is important in anaerobic conditions when there is no oxidative
phosphorylation to maintain the production of adenosine triphosphate
(ATP) by glycolysis

Posted by esraa hashim at Wednesday, September 09, 2009

Reactions: fun (0) attractive (1)

25 comments:

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