Intro To Med Chem Flashcards
a chemistry-based discipline, involving aspects of the
biological, medical and pharmaceutical scie
Medicinal Chemistry
is concerned with the invention, discovery, design,
identification and preparation of biologically active
compounds, the study of their metabolism, the interpretation
of their mode of action at the molecular level and the
construction of structure-activity relationships (SAR), which is
the relationship between chemical structure and
pharmacological activity for a series of compounds
Medicinal Chemistry
New active substances or drugs are identified and
prepared from natural sources, organic chemical reactions or
biotechnological processes. They are known as lead mole
Stage 1
Optimization of lead structure to improve potency,
selectivity and lessen toxicity
Stage 2
Development stage involves optimization of synthetic
route for bulk production and modification of pharmacokinetic
and pharmaceutical properties of active substance to render it
chemically useful
Stage 3
Cave paintings and symbolic artefacts found by archaeologists suggest the
earliest humans believed in spirits and supernatural forces. Primitive surgery,
trepanning, may have been to allow the evil spirits to leave a sick
Drugs of Antiquity
8000 BC: Prehistoric medicine
goddess Sekhmet was believed to cause or cure diseases and priests played
a large part in Egyptian medicine.
Papyrus- describe medical techniques similar to those used today
Egyptians used compression on a wound to stop bleeding and had
specialists in obstetrics and gynecology who were the forerunners of modern midwives
Drugs of Antiquity
2000 BC: Egyptian medicine
Emperor Shen Nung compiled a pharmacopeia which included ch’ang
shang and mahuang
American Indians used chaulmoogra fruit, coca leaves and mushrooms
Brazilians used ipecacuanha root
Greek apothecary shops sell opium, squill, Hyoscyamus and metallic drugs
Drugs of Antiquity
2000 BC
Empe
father of Modern Medicine
Hippocrates
Hippocrates – father of Modern Medicine; Hippocratic Oath
Romans realized the link between dirt and disease and developed
aqueducts to supply drinking water and sewers to remove wastes safely;
personal hygiene
Drugs of antiquity
450 BC to 300 AD
Paracelsus (1493-1541) glorified antimony and its salts as cure-all drug
Basic studies of chemistry and physics shifted from Greco-Roman to the
Arabian alchemists (between 13th
-16th century)
Materia Medica and pharmacopeias brought together traditional uses of
drugs
The Middle Ages
fall of the Roman Empire meant that many of their public hygiene practices
were soon lost
Medicine in the ages was dominated by religion; sickness =
punishment from God for sins committed; rise of monasteries as ‘hospitals’
Traditional cures, using herbal remedies and potions were seen as witchcraft and medicine
500 - 1400 AD: The Middle Ages
The Arabic world was the center of scientific and medical knowledge
Hippocrates’ theories and Islamic physician began to use the regulation of
diet, exercise and the prescription of medicinal herbs to treat their patient
Surgical operations were also performed and narcotic drugs were used as anesthetic
700 - 1500 AD: Arabic medicines
The middle ages
Poineer of vaccination
Edward jenner
led the understanding of infections caused by
bacteria or germs
Louis Pasteur & Robert Koch
Industrial revolution caused a massive change in people’s health
Many died due to cholera, TB, measles and pneumonia
Major medical advances: vaccinations and X-rays
1700 - 1900: Eighteenth and Nineteenth centuries
applied which led to a great advance in patient treatment: detailed observation, record-
keeping and the influence of environment to patient health
Ideas of Thomas Sydenham
18th and 19th centuries *
stry
Birth period of modern medicinal chemistry
Antoine Lavoisier’s works were refined and extended the techniques of
chemical analysis
Organic chemistry was staged by the synthesis of acetic acid by Kolbe (1845)
and methane by Berthelot (1856)
Pharmacognosy was replaced by physiologic chemistry
Emphasis was shifted from finding new medicaments from plants to finding
the active ingredients that accounted to their pharmacologic properties.
Increased use of “pure” substances as therapeutic agents
Isolation of morphine, emetine, caffeine, quinine and colchicine
The 19th Century: Age of Innovation and Chemistry