Current research efforts are now focused not only on discovering new biologically active compounds using ever increasingly sophisticated technology, but also on gaining a better understanding of how and where drugs exert their effects at the
Molecular level
Was defined by IUPAC specified commission as “it concerns the discovery, the development, the identification and the interpretation of the mode of action of biologically active compounds at the molecular level”
MEDICINAL CHEMISTRY
During the early stages of medicinal chemistry development, scientist was primarily concerned with the isolation of medicinal agents found in plants. Today, scientists in this field are also equally concerned with the
creation of new synthetic compounds as drugs
the structure of the synthetic drug must contain a (blank) component for us to have the idea that the compound can be absorbed, distributed, and excreted
hydrophobic and hydrophilic
Branches of Med Chem
Pharmacognosy
Pharmacology
Microbiology
Biochemistry
Bioinformatics
PHASES OF DRUG DISCOVERY
Phase I – Drug Discovery
Phase II – Drug Design
Phase III – Drug Testing and Development
Start: identifying a suitable drug
target
Knowledge of the (blank) played by that target allows the researcher to propose what effect a drug could have if it interacted with the target
physiological role
biological macromolecules (carbohydrates, lipids, enzymes, proteins, and nucleic acid)
Targets
Next: (blank) has to be developed
Suitable Testing Method
Drugs will demonstrate whether drugs have the desired activity
Suitable Testing Method
Finding a structure that will interact with the target Such structure is known as the
Lead structure
Phase II –
Drug design
Device synthetic routes that will allow the synthesis of various (blank) a compound having a structure similar to that of another compound, but differing from it in respect to a certain component
analog
Having produced a series of analogs, the activity of these compounds are compared and certain structural features that are more important to activity than others are identified
SAR
Phase III –
Drug Testing and Development
As soon as a potentially useful drug is discovered, it is then
patented
Thoroughly tested for any
side effects or toxicity
are carried out to identify what metabolites are formed
Drug metabolism
will then be tested for activity and side effects
Metabolites