Prelim (ALL)

• Medicinal chemistry, at the intersection of chemistry and pharmacology.
• Medicinal chemistry

  • plays a crucial role in the discovery and development of drugs.
• Ancient civilizations, such as the Egyptians, Greeks, and Chinese, relied heavily on herbal remedies for healing.
• Empirical knowledge

  • Medicinal knowledge that was based on observations and traditions.
• Paracelsus

  • Often regarded as the Father of Modern Pharmacology
• Paracelsus

  • he emphasized the use of chemistry in medicine
• Paracelsus

  • introduced the concept of dose-response relationships.
• Thomas Sydenham

  • contributed to the standardization of drug preparations, leading to the first pharmacopoeias.
• Isolation of morphine: Year 1805
• Friedrich Serturner

  • he isolated morphine from opium, marking the first isolation of an active compound.
• 1805

  • this year marks the first isolation of an active compound (morphine from opium).
• When (year) was Quinine isolated from the bark of the Cinchona tree?

  • 1820
• Quinine

  • isolated from the bark of the cinchona tree, it provided an effective treatment for malaria.
• When (year) was Urea synthesized?

  • 1828
• Friedrich Wohler

  • he synthesized urea from inorganic compounds, challenged the notion of vitalism, and laid the foundation for organic chemistry.
• When (year) were sulfonamide drugs developed?

  • 1930
• The development of sulfonamide drugs, such as Prontosil, marked the beginning of the pharmaceutical industry's engagement in drug discovery.
• When (year) was penicillin was discovered?

  • 1928
• Alexander Fleming

  • he discovered penicillin, and revolutionized antibiotic therapy.
• During this year, 1940 to 1960: The discovery of antibiotics, antipsychotics, and antihypertensives characterized a period of remarkable drug development.
• Random Screening Approach: The identification of new drugs relied on empirical approaches and random screening of natural and synthetic compounds.
• Structure-Based Drug Design: The elucidation of protein structures allowed for the design of drugs targeting specific molecular targets.
• Modern medicinal chemistry focuses on combination therapies, personalized medicine, and targeted therapies.
• Automation and high-throughput screening have expedited the drug discovery process.
• As medicinal chemistry advances, it is crucial to address ethical considerations related to drug development, access to treatments, and the responsible use of emerging technologies.
• Functional group

  • refers to a specific arrangement of atoms within a molecule that imparts characteristic chemical and often biological properties to that molecule.
• Functional group

  • These groups are responsible for the functional or reactive sites in a compound, influencing its reactivity, structure-activity relationship (SAR), and pharmacological properties.
• Understanding functional groups is crucial in drug design and medicinal chemistry, as it helps predict how a molecule will interact with biological targets and how changes to its structure may impact its biological activity.
• Hydroxyl group

  • is a vital component in many medicinal compounds, contributing to their solubility and reactivity.
• Hydroxyl group

  • It is a key feature in alcohols and phenols, influencing their pharmacological properties and therapeutic applications.
• Carbonyl group

  • is ubiquitous in medicinal chemistry, found in compounds such as ketones and aldehydes.
• Carbonyl group

  • Its presence imparts distinctive chemical reactivity and plays a pivotal role in the biological activity of various pharmaceutical agents.
• Amino group

  • is a fundamental constituent of amines and amino acids.
• Amino group

  • Its presence in medicinal compounds is essential for modulating pharmacokinetic parameters.
• Aromatic ring

  • is a hallmark of many bioactive compounds, endowing them with distinct molecular recognition capabilities and pharmacological profiles.
• Aromatic ring

  • Its presence in medicinal agents often correlates with enhanced binding affinity and therapeutic efficacy.
• Ester group

  • It is prevalent in numerous pharmaceuticals, influencing their metabolic stability and bioavailability.
• Ester group

  • Its role in drug design encompasses modulation of lipophilicity and enhancement of drug delivery properties.
• Drug-Receptor Interactions: Interactions between functional groups on a drug and complementary sites on a target receptor influence the drug's efficacy.
• Pharmacokinetics: Functional groups can affect a drug's absorption, distribution, metabolism, and excretion (ADME) properties.