Synthesis and Evaluation of Fluoroquinolone Derivatives Against M.Tuberculosis
碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所碩士班 === 95 === Tuberculosis (TB) is an ancient enemy of humans. The World Health Organization (WHO) estimates that one-third of the world’s population is infected by Mycobacterium tuberculosis. The association of TB and HIV infections has caused an urgent need in search o...
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| Format: | Others |
| Language: | zh-TW |
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2007
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| Online Access: | http://ndltd.ncl.edu.tw/handle/49244589212278875196 |
| Summary: | 碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所碩士班 === 95 === Tuberculosis (TB) is an ancient enemy of humans. The World Health Organization (WHO) estimates that one-third of the world’s population is infected by Mycobacterium tuberculosis. The association of TB and HIV infections has caused an urgent need in search of alternative chemotherapeutics for M. tuberculosis infection. We were particularly interested in the synthesis and evaluation of fluoroquinolones for their antibacterial activities.
The only position on the drug molecule where substitutions of bulky functional groups are permitted is at the 7-C ring position. The lipophilicity of the fluoroquinolones is well known to play an important role in the penetration of these compounds into bacterial cells.
Modification of three quinolones such as ciprofloxacin, ofloxacin and PD161141 are hope to provide more effective inhibitors of the enzyme with improved efficacy.
Dithiocarbamates has been demonstrated to possess antifungal and antibacterial properties. We had synthesized dithiocarbamate derivatives possessing different alkyl groups, in order to obtain new and potent antituberculosis compounds 5a-s and 8a-s.
These synthesized Quinolones derivatives evaluated for (1) antibacterial activity (especially against resistant strains); (2) anti-TB activity at Tuberculosis Antimicrobial Acquisition & Coordination (TAACF), U.S. National Institute of Allergy and Infectious Diseases.
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