Synthesis, biological evaluation and molecular docking of 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives as potential Staphylococcus aureus Sortase A inhibitors.

doi:10.1016/j.bmcl.2016.06.074

Paper

Synthesis, biological evaluation and molecular docking of 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives as potential Staphylococcus aureus Sortase A inhibitors.

Published Aug 15, 2016 · Yong Zhang, Jian Bao, Xin-Xian Deng

Bioorganic & medicinal chemistry letters

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18

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Abstract

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In Vitro Study

Study Snapshot

Novel 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives show excellent inhibitory activity against Staphylococcus aureus Sortase A, with the 7-position substituent being crucial for inhibitory activity.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis, biological evaluation and molecular docking of 2-phenyl-benzo[d]oxazole-7-carboxamide derivatives as potential Staphylococcus aureus Sortase A inhibitors.

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References

Sortase A Inhibitors: Recent Advances and Future Perspectives.

Sortase A inhibitors show potential as antivirulence drugs, preventing infections caused by Staphylococcus aureus and other Gram-positive bacteria.

Molecular basis of Streptococcus mutans sortase A inhibition by the flavonoid natural product trans-chalcone.

Trans-chalcone, a plant natural product, inhibits Streptococcus mutans sortase A and biofilm formation, suggesting potential as oral biofilm inhibitors.

Recent progress in the development of sortase A inhibitors as novel anti-bacterial virulence agents

SrtA inhibitors show promise as novel antibacterial agents against drug-resistant Gram-positive bacteria, offering a promising approach for developing new antibacterial drugs.

Targets for Combating the Evolution of Acquired Antibiotic Resistance

Understanding the molecular mechanisms of antibiotic resistance can help develop strategies to enhance our current antibiotic arsenal and combat antibiotic resistance.

Quercitrin, an Inhibitor of Sortase A, Interferes with the Adhesion of Staphylococcal aureus

Quercitrin, a natural compound, can inhibit Staphylococcus aureus's surface protein adhesion, potentially leading to new anti-virulence agents against infections.

Citations

Benzo[d]oxazoles from Anilides by N-Deprotonation–O-SNAr Cyclization

This study demonstrates a method for synthesizing benzo[d]oxazoles from anilide precursors, with high yields and temperature-dependent reactions depending on the C5 activating group on the SNAr acceptor ring.

DBU-Promoted Deaminative Thiolation of 1H-Benzo[d]imidazol-2-amines and Benzo[d]oxazol-2-amines.

This study developed a novel, environmentally friendly method for synthesis of various 2-thio-1H-benzo[d]imidazoles and 2-thiobenzo[d]oxazoles using carbon disulfide, offering potential applications in organic and medicinal chemistry.

Discovery of Sortase A covalent inhibitors with benzofuranene cyanide structures as potential antibacterial agents against Staphylococcus aureus.

Benzofuran cyanide derivatives with acrylonitrile moiety show potential as antibacterial agents against Staphylococcus aureus, with excellent inhibitory activity against SrtA and inhibitory effects on biofilm formation.

Identification of Novel Antistaphylococcal Hit Compounds Targeting Sortase A

Two novel antistaphylococcal compounds targeting sortase A were identified, both possessing antibacterial activity against multidrug-resistant Staphylococcus aureus strains.

Chemical Biology of Sortase A Inhibition: A Gateway to Anti-infective Therapeutic Agents.

Inhibiting sortase A activity offers a powerful anti-infective strategy without causing antibiotic-resistant strains, offering opportunities for medicinal chemists to combat antibiotic resistance.