- Synthesis and antibacterial activity of C2-symmetric binaphthyl scaffolded amino acid derivatives
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The synthesis of eleven novel antibacterial agents is reported. The structures are based on a C2-symmetric binaphthyl scaffold which holds two identical chains consisting of a short linker, a basic amino acid and a small hydrophobic side chain.
- Robertson, Mark,Bremner, John B.,Coates, Jonathan,Deadman, John,Keller, Paul A.,Pyne, Stephen G.,Somphol, Kittiya,Rhodes, David I.
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- De novo Design of SARS-CoV-2 Main Protease Inhibitors
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The COVID-19 pandemic prompted many scientists to investigate remedies against SARS-CoV-2 and related viruses that are likely to appear in the future. As the main protease of the virus, M Pro, is highly conserved among coronaviruses, it has emerged as a prime target for developing inhibitors. Using a combination of virtual screening and molecular modeling, we identified small molecules that were easily accessible and could be quickly diversified. Biochemical assays confirmed a class of pyridones as low micromolar noncovalent inhibitors of the viral main protease.
- Fischer, Christian,Vep?ek, Nynke A.,Peitsinis, Zisis,Rühmann, Klaus-Peter,Yang, Chao,Spradlin, Jessica N.,Dovala, Dustin,Nomura, Daniel K.,Zhang, Yingkai,Trauner, Dirk
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p. 458 - 463
(2021/10/16)
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- FACTOR XIIa INHIBITORS
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The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
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- Synthesis of a Novel Class of Peptides: Dilactam-Bridged Tetrapeptides
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As model compounds for the study of constrained peptides, the following lactam-bridged derivatives were synthesized: Ac-L--D--NHMe (I), Ac-L--L--NHMe (II), Ac-L--NHMe (III), Ac-L--D--NHMe (IV), Ac-L--L--NHMe (V), and Ac-L--NHMe (VI).Benzyloxycarbonyl and tert-butyloxycarbonyl groups were employed for amine protection and the benzyl and methyl esters for carboxyl protection.Coupling reactions were carried out by the use of active esters or through azide activation.Cyclization reactions were carried out by adding the active ester hydrochlorides into large volumes of pyridine at elevated temperatures.The cyclic intermediates were obtained in yields of 45-50percent.Fragment condensation of the cyclic dipeptides yielded the corresponding dilactam-bridged tetrapeptides.
- Manesis, Nick J.,Goodman, Murray
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p. 5331 - 5341
(2007/10/02)
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