MEDICINAL CHEMISTRY

A chemistry-based discipline, involving the aspects of biological, medical, and pharmaceutical science.

Medicinal chemistry encompasses ____, ____, ____, and ____.

Main driving force/highlight for medicinal chemistry

One of the first groups of drugs that was discovered thru medicinal chemistry

Metronidazole (Flagyl) is indicated as an ____.

Chemical compound that is used to treat, mitigate, diagnose, and prevent diseases both in humans and animals.

Compounds that interact with a biological system to produce a biological response - beneficial or toxic.

Chemical compound that has a pharmacologic or biological activity whose chemical structure is used as a starting point for chemical modification in order to improve potency, selectivity, or pharmacokinetics parameters.

Lead compounds thar underwent modifications.

Innovative or new drugs for previously unmet medical needs

Drugs for rare medical conditions

Ideal drug that is free from side effects

Compound that undergoes biotransformation prior to exhibiting its pharmacological effects

2 Broad categories of prodrugs

Consist of the attachment of a carrier group to the active drug to alter its physicochemical properties and the subsequent enzymatic or non-enzymatic mechanisms to release the active drug moiety Ex: Macromolecules

Compounds that already contain the embryo of the active species within their structure.

IDENTIFY THE PRODRUG CATEGORY. Inactive prontosil reduction to sulphanilamide (anti-bacterial)

IDENTIFY THE PRODRUG CATEGORY. Inactive cyclophosphamide oxidation to phosphoramide mustard (antineoplastic)

Mechanism of action of phosphoramide mustard

2 Other terms for double prodrug

Carried out by enzymatic conversion to prodrug is possible before the “pro-drug” release the active ingredient

Prodrugs that use macromolecules as carriers

Carrier acts as transporter of the active drug to a specific targeted site

Example of a site-specific prodrug liberated in the colon