The 4-Quinolone-3-Carboxylic Acid Motif as a Multivalent Scaffold in Medicinal Chemistry

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Quinolones are among the most common frameworks present in the bioactive molecules and hence represent an attractive starting point for the design of combinatorial libraries. Since 1962 4-quinolone-3-carboxylic acid derivatives are clinically used as antibacterial agents worldwide. Currently, fluoroquinolones are approved by the WHO as second-line drugs to treat tuberculosis (TB), and their use in multidrug-resistant (MDR)-TB is increasing due to the fact that they have a broad and potent spectrum of activity and can be administered orally. In the last years, quinolones endowed with “nonclassical” biological activities, such as antitumor, anti-HIV-1 integrase, cannabinoid receptor 2 agonist/antagonist activities, have been reported by our research group as well as by other researchers. This review focuses on the 4-quinolone-3- carboxylic acid motif as a privileged structure in medicinal chemistry for obtaining new compounds possessing antibacterial, antitumor, anti-HIV, and cannabinoid receptors modulating activities. Synthetic approaches, structure-activity relationships, mechanisms of action, and therapeutic potentials of these novel classes of pharmacologically active compounds are presented.

Keywords: CB2 agonists; HIV-1 integrase inhibitors; Quinolones; anti-tumor agents; drug design; privileged structure

Document Type: Research Article


Affiliations: Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena Via A. Moro, snc 53100 Siena, Italy.

Publication date: May 1, 2009

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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