Indole/isatin-containing hybrids as potential antibacterial agents
Feng Song1,2, Zhenghua Li1, Yunqiang Bian1
1Shandong Key Laboratory of Biophysics, Institute of Biophysics, Dezhou University, Dezhou, Shandong, China.
Archiv Der Pharmazie
|July 16, 2020
Summary
Novel indole/isatin hybrids show promise as antibacterial drug candidates against resistant bacteria. This review highlights their development and structure-activity relationships for future drug design.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- The rise of drug-resistant bacteria necessitates new antibacterial agents.
- Indole and isatin derivatives are versatile scaffolds with diverse pharmacological activities.
- Indole/isatin hybrids show potential against key bacterial pathogens.
Purpose of the Study:
- To review the development of indole/isatin hybrids as antibacterial agents.
- To analyze the structure-activity relationships (SAR) of these compounds.
- To guide the rational design of novel antibacterial drug candidates.
Main Methods:
- Literature review of articles published from January 2015 to May 2020.
- Analysis of synthetic strategies for indole/isatin hybrids.
- Evaluation of reported antibacterial activities and SAR data.
Main Results:
- Indole/isatin hybrids exhibit significant activity against Gram-positive and Gram-negative bacteria.
- Specific structural modifications correlate with enhanced antibacterial efficacy.
- SAR studies provide insights into key pharmacophoric features.
Conclusions:
- Indole/isatin hybrids represent a promising class of compounds for combating bacterial infections.
- Further research into SAR can optimize lead compounds for clinical development.
- These scaffolds offer a viable strategy for discovering next-generation antibiotics.
More Related Videos
Related Concept Videos
01:27Combined Effects of Drugs: Synergism
6.6K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
6.6K
00:57Antibiotic Selection
58.9K
Overview
58.9K
01:28Antimicrobial Effectiveness
826
The effectiveness of antimicrobial agents depends on various factors influencing their ability to eliminate microbial populations. Larger microbial populations require more time for complete eradication, emphasizing the importance of population size analysis when evaluating antimicrobial efficacy.Microbial resistance to antimicrobial agents varies significantly. Highly resilient microorganisms include endospores, gram-negative bacteria, and non-enveloped viruses, while prions are exceptionally...
826
01:11Aryldiazonium Salts to Azo Dyes: Diazo Coupling
3.5K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para...
3.5K
02:07FISH - Fluorescent In-situ Hybridization
23.4K
Fluorescence in situ hybridization, or FISH, was developed in the early 1980s and has quickly become one of the most widely used techniques in cytogenetics. Labeled probes are used to bind complementary DNA or RNA sequences on a chromosome or in a region within a cell. Earlier, the probes could only be obtained by cloning or reverse transcription of a DNA template. Currently, the probe oligonucleotides can be synthesized synthetically. Additionally, with the advancement of optical techniques,...
23.4K
01:27Chemical Agents for Microbial Control
641
Chemicals play important roles in controlling microbial growth by targeting microbial structures and functions as sanitizers, antiseptics, disinfectants, and sterilants.Alcohols are commonly used sanitizers, effectively disrupting lipid membranes, which compromises cell integrity. They are also used as antiseptics and disinfectants due to their rapid action and versatility.Phenols and their derivatives phenolics , known for denaturing proteins and disrupting cell membranes, are particularly...
641