Overview of Medicinal Chemistry

Overview of Medicinal Chemistry

• Medicinal chemistry was coined after World War II, but the use of chemicals for medicinal purposes dates back to ancient times.
• Ancient people recognized healing properties in plants without understanding their mechanisms of action.
• Examples of ancient herbal remedies include ginseng for respiratory issues in ancient China and willow bark for pain relief in ancient Egypt and Sumeria.
• Paracelsus in the Renaissance was a pioneer in using alchemy to discover the medicinal use of chemicals, like mercury and antimony.
• Louis XIV's use of antimony for digestive issues marked an important step.
• The 1900s saw the rise of modern medicinal chemistry with Aspirin as the first synthetic drug for pain relief.
• World War I and II prompted research in chemical synthesis leading to significant advancements in antibiotics (sulfa drugs, Prontosil, and penicillin).
• Modern medicinal chemistry has advanced beyond the initial focus of painkillers and antibiotics to include hormonal drugs, contraceptives, antiviral drugs, and cancer treatments.

Traditional Medicine

• Traditional medicine (TM) encompasses diverse health practices globally.
• TM has been used for centuries, especially in primary healthcare at the community level, in both developed and developing countries.
• TM's richness is tied to civilizations' histories, with Chinese, Indian, and Iranian systems being particularly comprehensive.
• TM includes herbal medicine, which was crucial for discoveries such as ephedrine and artemisinin.
• In western countries, adaptations of TM are sometimes called "alternative" or "complementary" medicine.

Alternative Medicine

• Alternative medicine encompasses diverse practices outside conventional medicine.
• These practices include folk medicine, herbal remedies, homeopathy, Ayurveda, chiropractic, acupuncture, and naturopathy.
• Alternative medicine's popularity is linked to patients' values and beliefs, providing more personal autonomy.

The Formulation of the First Antibiotics

• Alexander Fleming's discovery of penicillin in 1928 revolutionized medicine by providing an effective treatment for bacterial infections.
• Collaborating with other scientists, like Howard Florey and Ernst Boris Chain, led to mass penicillin production.

The First Vaccine

• Edward Jenner developed the smallpox vaccine in 1796, setting a precedent for immunology.
• Louis Pasteur's developments of rabies and anthrax vaccines solidified the principle of using attenuated organisms for disease prevention.

Major Breakthroughs in Vaccines

• The development of vaccines substantially reduced disease prevalence.
• Advancements in tissue culture and microbiology facilitated vaccine development for polio, measles, mumps, rubella, and varicella.
• Vaccines for hepatitis B and Haemophilus influenzae type b marked further progress.

The COVID-19 Vaccine

• The COVID-19 pandemic spurred the development of gene-based and protein-based vaccines.
• Significant success was seen with mRNA vaccines from Pfizer-BioNTech.
• Addressing vaccine hesitancy and ensuring broad vaccine coverage are crucial for pandemic response.

Hit Compounds

• Many modern pharmaceutical compounds are based on natural compounds from organisms.
• Hit compounds are those identified via screening processes due to specific bioactivity.
• Development often involves multiple trials to determine compound efficacy and safety.
• Examples include artemisinin (for malaria) and alpha-mangostin (for dengue).

Global Trends in Reported Paralytic Polio, Measles, and Tetanus Cases (1980-2023)

• Vaccines significantly reduced the prevalence of polio, measles, and tetanus.
• Polio saw the most rapid decline, whereas measles had periodic outbreaks.
• Tetanus, a persistent environmental disease, also saw a decline.
• Continued vaccination is essential for disease control, especially in areas with limited access to health care.

Current Government Project on Pharmaceutical and Drug Discovery

• PEZA, FDA, and OSAPIEA are collaborating in the Philippines to enhance pharmaceutical and medical device manufacturing.
• The "Tuklas Lunas Program" is another key government initiative harnessing natural resources for drug discovery and development.
• These initiatives aim to lower drug costs, create jobs, and promote healthcare independence in the Philippines.

Health Inequities in the Philippines

• High medication costs and reliance on imported drugs are concerns in the Philippines.
• This particularly impacts rural areas, and low-income households.
• Generic drug availability and affordability issues also affect access in public health facilities and among Indigenous Peoples.

Antimicrobial Resistance

• Misuse/overuse of antimicrobials in healthcare, agriculture, and industry contribute to antimicrobial resistance development.
• Genetic material mutations, permeability changes, and gene transfer are key mechanisms of resistance.

Importance of Continued Antibiotic Research

• Continued research for new drugs and treatments is crucial due to the prevalence and persistence of antimicrobial resistance problems.