Organic Pharmaceutical Chemistry: Prodrugs 1

Organic Pharmaceutical Chemistry IV
1st Semester, Year 5 (2016-2017)
Lecture 1



Organic Pharmaceutical Chemistry:
Prodrugs




Dr Asim A. Balakit
Pharmaceutical Chemistry Dept.,
College of Pharmacy,
Babylon University

This lecture is mainly based on:
http://shodhganga.inflibnet.ac.in/bitstream/10603/3457/10/10_chapter%201.pdf

History & Basic Concept

The prodrug concept was first proposed by Albert in 1958.

Albert and his co-workers described prodrugs as pharmacologically inactive chemical derivatives that could be used to alter the physicochemical properties of drugs, in a temporary manner, to increase their usefulness and/or to decrease associated toxicity.

This included both compounds that are designed to undergo a transformation to yield an active substance and those that were discovered by serendipity to do so.

These two situations were distinguished by Harper, who in 1959 introduced the term drug Iatentiation to refer to drugs that were specifically designed to require bioactivation.