AI Article Synopsis
- A series of modified fluoroquinolone derivatives (gatifloxacin, ciprofloxacin, and 8-OCH(3) ciprofloxacin) were created to enhance their lipophilicity, characterized using various analytical techniques.
- While these new derivatives showed decreased effectiveness against Mycobacterium smegmatis compared to their parent compounds, one specific compound (compound 6) demonstrated significantly greater potency against MTB H37Rv, outperforming several well-known antibiotics.
- The findings suggest that improving lipophilicity alone isn’t enough to enhance antimycobacterial activity, indicating other factors are involved.
Article Abstract
A series of gatifloxacin, ciprofloxacin, and 8-OCH(3) ciprofloxacin coumarin derivatives with remarkable improvement in lipophilicity as compared to the parent fluoroquinolones was designed, synthesized, and characterized by (1) H-NMR, MS, and HRMS. These derivatives were evaluated for their in-vitro activity against Mycobacterium smegmatis CMCC 93202 and MTB H37Rv ATCC 27294. All of the synthesized compounds were less active than the parent compounds against M. smegmatis CMCC 93202, but the activity of compound 6 was found to be 2-8-fold more potent than ciprofloxacin, 8-OCH(3) ciprofloxacin, moxifloxacin, and rifampin, and comparable to gatifloxacin against MTB H37Rv ATCC 27294. These results indicated that the lipophilicity of the tested compounds is not the sole parameter affecting antimycobacterial activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/ardp.201000256 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!