Project Details Review of stand alone drugs

Project No.:
2005-032-2-700
Start Date:
20 December 2005
End Date:
01 July 2010
Division Name:
Chemistry and Human Health Division
Division No.:
700

Objective

The project will study drugs having no structural and pharmacological analogues. In several cases it is not possible to improve an existing drug with the help of analogues. The “Stand Alone Drugs” will be studied among the most frequently used drugs (e.g. Top 500 drugs). The project will afford a review article on them.

Description

Acetylsalicylic acid is one of the oldest small molecule drugs, which is at the same time a "Stand Alone Drug" having a specific property as an irreversible inhibitor of COX-1 enzyme. Several efforts tried to improve acetylsalicylic acid with the help of analogue-based research. These efforts remained unsuccessful. The same is true in several other Stand Alone Drugs, such as diltiazem (L-type calcium antagonist), levodopa (dopamine pro-drug) etc.

Analogue-based Drug Discovery (ABDD) has been the most successful direction in drug research. An IUPAC project studied this field and a book was published in January 2006 on this topic as a result of the IUPAC project. (see reference) This successful approach of the drugs research has, however, limitations. To the limitations of the ABDD belong the "Stand Alone Drugs", whose analogue-based modifications did not afford new drugs.

The aim of the project "Review of Stand Alone Drugs" will identify these drugs among the most frequently used drugs (e.g. Top 500 drugs) and their role on medicinal chemistry will be studied. Identification of Stand Alone Drugs will help the orientation among the drugs, because stand alone drugs and analogues represent the two main fields among the drugs. Drugs without known mechanism of action are out of the scope of this study.

Progress

* project announcement published in Chem. Int. Sep 2008

July 2010 – project completed - The outcome of this project is as chapter 2 in a book published by Wiley-VCH, Weinheim, Analogue-based Drug Discovery II – see project 2008-013-1-700

This book chapter is published online (free access):  https://onlinelibrary.wiley.com/doi/10.1002/9783527630035.ch2/summary