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

$63.10 plus tax (Refund Policy)

Buy Article:

Abstract:

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

DOI: http://dx.doi.org/10.2174/092986709788186156

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

Publication date: May 1, 2009

More about this publication?
  • 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.
Related content

Tools

Favourites

Share Content

Access Key

Free Content
Free content
New Content
New content
Open Access Content
Open access content
Subscribed Content
Subscribed content
Free Trial Content
Free trial content
Cookie Policy
X
Cookie Policy
ingentaconnect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more