Abstract
One of the most important stages of the drug discovery process is the generation of lead compounds. Structure-activity relationships (SAR) are well-integrated in modern drug discovery and have been largely used for the finding of new leads, scaffold generation, the optimization of receptor or enzyme affinity, as well as of pharmacokinetic and physicochemical properties. This review highlights some SAR approaches that can be used to optimize leads through a continuous, multi-step process based on knowledge gained at each stage, thus exploiting SAR in the design of selective, potent, small-molecule drug candidates.
Keywords: sar, drug design, enzyme inhibitors, cox, protein kinase, qsar, adme
Mini-Reviews in Medicinal Chemistry
Title: Structure-Activity Relationships for the Design of Small-Molecule Inhibitors
Volume: 5 Issue: 6
Author(s): Adriano D. Andricopulo and Carlos A. Montanari
Affiliation:
Keywords: sar, drug design, enzyme inhibitors, cox, protein kinase, qsar, adme
Abstract: One of the most important stages of the drug discovery process is the generation of lead compounds. Structure-activity relationships (SAR) are well-integrated in modern drug discovery and have been largely used for the finding of new leads, scaffold generation, the optimization of receptor or enzyme affinity, as well as of pharmacokinetic and physicochemical properties. This review highlights some SAR approaches that can be used to optimize leads through a continuous, multi-step process based on knowledge gained at each stage, thus exploiting SAR in the design of selective, potent, small-molecule drug candidates.
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Cite this article as:
Andricopulo D. Adriano and Montanari A. Carlos, Structure-Activity Relationships for the Design of Small-Molecule Inhibitors, Mini-Reviews in Medicinal Chemistry 2005; 5 (6) . https://dx.doi.org/10.2174/1389557054023224
DOI https://dx.doi.org/10.2174/1389557054023224 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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