期刊
CURRENT MEDICINAL CHEMISTRY
卷 16, 期 14, 页码 1746-1767出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/092986709788186156
关键词
Quinolones; HIV-1 integrase inhibitors; anti-tumor agents; CB2 agonists; drug design; privileged structure
资金
- Ministero dell'Universita della Ricerca [Prot. N 2006030948_002]
- University of Siena
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.
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