History of Chemical Synthesis Flashcards
What defines the Pharmaceutical Industry?
It is a commercial business focused on researching, developing, marketing, and distributing drugs, often subject to strict regulations concerning patenting, testing, and marketing.
Who are ‘Big Pharma’ and ‘Biotech’ companies?
‘Big Pharma’ refers to large companies with significant revenue and R&D expenditure, while ‘Biotech’ companies are often university spin-offs funded by venture capital and may collaborate with or be acquired by Big Pharma.
What is Medicinal Chemistry?
A scientific discipline involving the design, synthesis, and development of drugs, often requiring interdisciplinary knowledge in fields such as organic chemistry, pharmacology, and molecular biology.
What is the Structure-Activity Relationship (SAR) in drug development?
SAR is the process of correlating a drug’s chemical structure with its biological activity, aiming to optimize therapeutic effects through structural modifications.
What are some key historical milestones in early drug discovery?
- ca. 60,000 B.C.: Use of plants for medicinal purposes in Iraq.
- 4,000 B.C.: Sumerians used laurel and thyme for health.
- 2,700 B.C.: Shennong Bencao Jing (Chinese herbal book) documents 365 medicinal plants.
What was the significance of Paracelsus in the 16th century?
Paracelsus challenged herbal medicine, advocating for chemical medicines and seeking the ‘healing essence’ in pharmaceuticals.
How did William Withering contribute to drug discovery?
In 1785, he ground foxglove (digitalis) to treat heart conditions, essentially conducting an early clinical trial on 158 patients to establish an effective and safe dose.
What is Lipinski’s Rule of Five?
A set of guidelines for drug-likeness stating that orally active drugs should have: ≤5 hydrogen bond donors, ≤10 hydrogen bond acceptors, MW < 500 Da, and ClogP < 5.
How did synthetic chemistry progress in the 19th century?
Key advancements included Friedrich Wöhler’s synthesis of urea (1828) and William Perkin’s discovery of the mauveine dye (1856), which indirectly fostered the pharmaceutical industry.
What are high-throughput screening (HTS) and virtual high-throughput screening (VHTS)?
HTS is a method of quickly testing large libraries of compounds for activity against a target, while VHTS uses computer modeling to simulate this screening process.
Describe the stages of clinical trials in drug development.
- Phase I: Safety and dosage in healthy volunteers.
- Phase II: Efficacy and side effects in patients.
- Phase III: Large-scale testing for efficacy and monitoring for adverse reactions.
- Phase IV: Post-marketing surveillance.
What role does ADME play in pharmacokinetics?
ADME (Absorption, Distribution, Metabolism, Elimination) determines a drug’s movement and effects in the body, impacting dose, effectiveness, and safety.
What are some essential physicochemical properties in drug design?
These include solubility, size, lipophilicity, melting point, number of hydrogen bond donors/acceptors, and rotatable bonds, which affect the drug’s success.
What are the 12 Principles of Green Chemistry?
Guidelines for sustainable chemistry, including waste prevention, atom economy, less hazardous synthesis, use of renewable feedstocks, and safe chemical design.
What are enabling technologies in drug discovery?
Techniques like electrochemistry, photochemistry, and flow chemistry that enable new synthetic pathways, improve efficiency, and enhance safety.
