scholarly journals Aloe-emodin derived azoles as a new structural type of potential antibacterial agents: design, synthesis, and evaluation of the action on membrane, DNA, and MRSA DNA isomerase

2021 ◽  
Vol 12 (4) ◽  
pp. 602-608
Author(s):  
Xin-Yuan Liang ◽  
Narsaiah Battini ◽  
Yan-Fei Sui ◽  
Mohammad Fawad Ansari ◽  
Lin-Ling Gan ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Structural Type ◽  
Bacterial Membrane ◽  
Design Synthesis ◽  
Aloe Emodin

Tetrazole aloe-emodin 4b displayed potent efficacy against MRSA, and it was found to rapidly permeate the bacterial membrane to intercalate into DNA and form supermolecule with MRSA DNA isomerase (PDB code: 2XCS).

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Energy Coupling ◽  
Coupling Factor ◽  
Design Synthesis ◽  
Screening Design ◽  
Starting Point ◽  
Wide Range ◽  
Vitamin Uptake

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>

Design, Synthesis, and Structure−Activity Relationships of Benzophenone-Based Tetraamides as Novel Antibacterial Agents

2009 ◽  
Vol 52 (16) ◽  
pp. 5020-5031 ◽  
Author(s):  
Sunil K. Vooturi ◽  
Chrissy M. Cheung ◽  
Michael J. Rybak ◽  
Steven M. Firestine
Keyword(s):  
Antibacterial Agents ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity

Design, synthesis and evaluation of phenylthiazole and phenylthiophene pyrimidindiamine derivatives targeting the bacterial membrane

2020 ◽  
Vol 190 ◽  
pp. 112141
Author(s):  
Tingting Fan ◽  
Weikai Guo ◽  
Ting Shao ◽  
Wenbo Zhou ◽  
Pan Hu ◽  
...  
Keyword(s):  
Bacterial Membrane ◽  
Design Synthesis

Design, synthesis and biological evaluations of quaternization harman analogues as potential antibacterial agents

2018 ◽  
Vol 160 ◽  
pp. 23-36 ◽  
Author(s):  
Jiangkun Dai ◽  
Wenjia Dan ◽  
Siyu Ren ◽  
Congguo Shang ◽  
Junru Wang
Keyword(s):  
Antibacterial Agents ◽  
Design Synthesis

Design, Synthesis, and Biological Evaluation of Hexacyclic Tetracyclines as Potent, Broad Spectrum Antibacterial Agents

2015 ◽  
Vol 58 (11) ◽  
pp. 4703-4712 ◽  
Author(s):  
Cuixiang Sun ◽  
Diana K. Hunt ◽  
Chi-Li Chen ◽  
Yonghong Deng ◽  
Minsheng He ◽  
...  
Keyword(s):  
Broad Spectrum ◽  
Antibacterial Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation
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