Antibiotics 2012, 1(1), 1-13; doi:10.3390/antibiotics1010001
Classification Framework and Chemical Biology of Tetracycline-Structure-Based Drugs
1
Italian National Board of Chemists and Italian Chemical Society, Rome, 00187, Italy
2
McGill Nutrition and Performance Laboratory, Department of Oncology, School of Medicine, McGill University, 5252 Maisonneuve Street, Montreal, QC, H4A3S5, Canada
Received: 2 May 2012 / Revised: 21 May 2012 / Accepted: 8 June 2012 / Published: 12 June 2012
Abstract
By studying the literature about tetracyclines (TCs), it becomes clearly evident that TCs are very dynamic molecules. In some cases, their structure-activity-relationship (SAR) are well known, especially against bacteria, while against other targets, they are virtually unknown. In other diverse fields of research—such as neurology, oncology and virology—the utility and activity of the tetracyclines are being discovered and are also emerging as new technological fronts. The first aim of this paper is to classify the compounds already used in therapy and prepare the schematic structure that includes the next generation of TCs. The second aim of this work is to introduce a new framework for the classification of old and new TCs, using a medicinal chemistry approach to the structure of those drugs. A fully documented Structure-Activity-Relationship (SAR) is presented with the analysis data of antibacterial and nonantibacterial (antifungal, antiviral and anticancer) tetracyclines. The lipophilicity and the conformational interchangeability of the functional groups are employed to develop the rules for TC biological activity.Keywords:
tetracycline; anthracycline; aminomethylcycline; CMT; fuorocycline; pentacycline; antibiotics; non-antibiotics
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MDPI and ACS Style
Fuoco, D. Classification Framework and Chemical Biology of Tetracycline-Structure-Based Drugs. Antibiotics 2012, 1, 1-13.
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