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Antibiotics 2012, 1(1), 1-13; doi:10.3390/antibiotics1010001
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Classification Framework and Chemical Biology of Tetracycline-Structure-Based Drugs

1,2
Received: 2 May 2012; in revised form: 21 May 2012 / Accepted: 8 June 2012 / Published: 12 June 2012
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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 tetracycline; anthracycline; aminomethylcycline; CMT; fuorocycline; pentacycline; antibiotics; non-antibiotics
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

AMA Style

Fuoco D. Classification Framework and Chemical Biology of Tetracycline-Structure-Based Drugs. Antibiotics. 2012; 1(1):1-13.

Chicago/Turabian Style

Fuoco, Domenico. 2012. "Classification Framework and Chemical Biology of Tetracycline-Structure-Based Drugs." Antibiotics 1, no. 1: 1-13.


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