COMPREHENSIVE PMOC/DDD

FROM THE PPT ITSELF (AND SIDE NOTES)

Devoted to the discovery and development (organic, analytical, and

biochemical aspects) of new agents for treating diseases

Medicinal Chemistry

target brain infections: dapat highly lipophilic (can cross bbb)

Physicochemical properties

gout (mataas ang uric acid), we need to inhibit xanthine oxidase

Mechanism of Action

cyclophosphamide (pro drug), an anti cancer that can activated as phosphosamide mustard and metabolize acrolein (toxic)

Drug Metabolism and the activities of its metabolites

Structure

Stereochemistry

Hindi pwedeng masira / modify = hindi na marerecognize ng receptor thus not elicit desired effects

Pharmacophore

Drug carrier

Pharmacophore

Light carrier

Phosphorus

It is the region of a molecule containing the essential organic functional groups that directly interact with the receptor active site, therefore, conferring the biologic activity of interest.

Pharmacophore

A part of a molecular structure that is responsible for a particular biological or pharmacologic interaction that it undergoes

Pharmacophore

Can target microbial and cancer cells

Local Anti-infectives

a drug treatment that can kill or inhibit the growth of cells

Chemotherapy

According on the target cell: microbial cells

Antimicrobials

According on the target cell: cancer cells

Antineoplastics

According sa effect: they kill cells

Bacteriocidal

According sa effect: they inhibit the growth of the cells

Bacteriostatic

“Father of Antiseptic Surgery”

Joseph Lister

They used this for mouthwash before

Phenol

problem: after surgery madami namamatay and infections from one patient to another, continuous lang

Antiseptic

Introduced antiseptic principles for use in surgery and post-traumatic injury

Joseph Lister

Used phenol (carbolic acid)

Joseph Lister

The practice resulted in a significant decrease in the incidence of postsurgical infections.

Joseph Lister

“Father of Handwashing”

Ignaz Semmelweis

“Father of Chemotherapy”

Paul Ehrlich

Began work with antibacterial dyes and arsenicals

Paul Ehrlich

Discovered Salvarsan (An anti-syphilis drug)

Paul Ehrlich

Salvarsan also known as?

Compound 606 / Arsphenamine

What is the element within Salvarsan

Arsenic

Caused by treponema pallidum

Syphillis drug

Selective toxicity principle

Paul Ehrlich

Toxic lang sa mismong microbes, hindi sa mismong host

Selective toxicity principle

Local: sa site of action lang ang effects

Germicides

Anti-infective agents that are used locally

Germicides

Compounds that kill (-cidal) or prevent the growth of (-static) microorganisms when applied to living tissue

Antiseptic

alcohol on a human’s hand: antiseptic

Antiseptic

An agent that prevents transmission of infection by the destruction of pathogenic microorganisms when applied to inanimate objects.

Disinfectant

Non living things

Disinfectant

Local Anti-Infectives

 Alcohols and Related Compounds

 Phenols and Their Derivatives

 Oxidizing Agents

 Halogen-Containing Compounds

 Cationic Surfactants

 Dyes

 Mercury Compounds (Mercurials)

 Preservatives

ALCOHOLS AND RELATED COMPOUNDS