Design and Synthesis of Pyrrolidine-based Fragments That Sample Three-dimensional Molecular Space.
Sign Up to like & getrecommendations! Published in 2019 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00070
Abstract: Fragment-based drug discovery (FBDD) is a well-established technology for lead compound generation in drug discovery. As this technology has evolved, the design of fragments for screening has also evolved to engender not just an understanding… read more here.
Keywords: pyrrolidine based; design synthesis; based fragments; synthesis pyrrolidine ... See more keywords
N-Phosphorylated Pyrrolidines: An Overview of Synthetic Approaches
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DOI: 10.1055/s-0039-1690889
Abstract: Organophosphorus pyrrolidine derivatives possessing P–N bonds are a promising yet underexplored class of compounds. In this short review we overview the general approaches to these compounds described so far, with a special emphasis on their… read more here.
Keywords: pyrrolidines overview; pyrrolidine based; pyrrolidine; phosphorylated pyrrolidines ... See more keywords
Determinants for α4β2 vs. α3β4 Subtype Selectivity of Pyrrolidine-Based nAChRs Ligands: A Computational Perspective with Focus on Recent cryo-EM Receptor Structures
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DOI: 10.3390/molecules26123603
Abstract: The selectivity of α4β2 nAChR agonists over the α3β4 nicotinic receptor subtype, predominant in ganglia, primarily conditions their therapeutic range and it is still a complex and challenging issue for medicinal chemists and pharmacologists. Here,… read more here.
Keywords: subtype selectivity; pyrrolidine based; determinants subtype; receptor ... See more keywords
Synthesis of pyrrolidine-based hamamelitannin analogues as quorum sensing inhibitors in Staphylococcus aureus
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DOI: 10.3762/bjoc.14.260
Abstract: Interfering with bacterial cell-to-cell communication is a promising strategy to combat antimicrobial resistance. The natural product hamamelitannin and several of its analogues have been identified as quorum sensing inhibitors. In this paper the synthesis of… read more here.
Keywords: synthesis pyrrolidine; pyrrolidine based; hamamelitannin; quorum sensing ... See more keywords