Design, synthesis and antibacterial activity evaluation of moxifloxacin-amide-1,2,3-triazole-isatin hybrids

Clicks: 571
ID: 50535
2019
Article Quality & Performance Metrics
Overall Quality Improving Quality
84.7 /100
Combines engagement data with AI-assessed academic quality
AI Quality Assessment 🥈 High Quality
83.0 /100
Academic Rigor 88.0%
Novelty 78.0%
Clarity 87.0%
Key Strengths
  • Novel hybrid compound design
  • Comprehensive antibacterial activity evaluation
  • Identification of promising lead compounds (7e, 7g, 7j)
Areas for Improvement
  • Poor in vivo pharmacokinetic profiles of lead compounds
  • Limited cytotoxicity assessment (only CHO cells)
  • Lack of detailed mechanism of action studies
AI Recommendations

Further investigation into improving the pharmacokinetic properties of the lead compounds is crucial. Expanding the cytotoxicity assessment to include a wider range of cell lines would strengthen the safety profile. Exploring the mechanism of action of the hybrids could provide valuable insights for future drug design.

Enhanced v2.0 Analysis NISO/DORA Compliant
NISO/DORA Compliant
High Impact
📊 Established
Topic Trend
2025 Relevance
Relevance
0%
Importance
0%
Authorship
Unknown
Authors
0
Diversity
0%
Research Integrity
COPE Standards
Integrity
0%
Innovation
0%
Interdisciplinary Value
🔀 Cross-disciplinary
68%
Practical Impact Potential
Real-world Applications
75%
Enhanced Evaluation v2.0: Following NISO RP-25-2016, DORA 2025, and COPE assessment standards with 13 quality dimensions.
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Ranked #10 of 133 articles by views in Bioorganic chemistry

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Abstract
In this work, a series of novel moxifloxacin-amide-1,2,3-triazole-isatin hybrids 7a-l were designed and synthesized. The in vitro antibacterial activity against a panel of clinically important Gram-positive and Gram-negative bacteria including drug-resistant pathogens was also evaluated. All hybrids showed considerable activity against the tested pathogens with MIC values of ≤0.03 to 128 μg/mL, and some of them such as hybrids 7e, 7g and 7j were comparable to or better than the parent moxifloxacin (MIC: ≤0.03-8 μg/mL). Moreover, hybrids 7e, 7g and 7j also demonstrated low cytotoxicity towards CHO cells. However, the in vivo pharmacokinetic profiles of these three hybrids were generally far inferior to the parent moxifloxacin. The structure-activity relationship and structure-cytotoxicity relationship were also studied and discussed which may help with the identification of new chemical entities as potent antibacterial agents.
Reference Key
gao2019designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Gao, F.
Journal Bioorganic chemistry
Year 2019
DOI
10.1016/j.bioorg.2019.103162
URL
Keywords Keywords not found

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