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A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design.
The role of sulfur interactions in protein structure and function is discussed and although relatively rare, intermolecular interactions between ligand C-S σ* orbitals and proteins are illustrated. Expand
Actin-binding marine macrolides: total synthesis and biological importance.
This review summarizes the biological properties of these unusual marine natural products and features the recently completed total syntheses of swinholide A, scytophycin C, aplyronine A, mycalolide A--all of these being potent cytotoxic agents that target actin--and a diastereoisomer of ulapualide A. Expand
Phosphocholine Conjugation: An Unexpected In Vivo Conjugation Pathway Associated with Hepatitis C NS5B Inhibitors Featuring A Bicyclo[1.1.1]Pentane
The participation in xenobiotic metabolism of a process whose function is ordinarily limited to the synthesis of endogenous compounds is demonstrated, and concerns about the possibility that compounds 1 and 2 might interfere with routine phospholipid synthesis are raised. Expand
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase.
Structural-activity relationship studies resulted in the optimization of the activity of members of a class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors, and analogues exhibiting improved solubility and membrane permeability were shown to have notably enhanced pharmacokinetic profiles. Expand
A base-catalyzed, direct synthesis of 3,5-disubstituted 1,2,4-triazoles from nitriles and hydrazides
A convenient and efficient one step, base-catalyzed synthesis of 3,5-disubstituted 1,2,4-triazoles by the condensation of a nitrile and a hydrazide is presented. A diverse range of functionality andExpand
Friedel–Crafts acylation of indoles in acidic imidazolium chloroaluminate ionic liquid at room temperature
Abstract A practical and convenient protocol has been developed for the acidic 1-ethyl-3-methylimidazolium chloroaluminate ionic liquid (generated from 1-ethyl-3-methylimidazolium chloride (EmimCl)Expand
Structure-activity relationship studies of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of HCV NS3 serine protease.
A survey of isosteric replacements of the phosphonoalanine side chain coupled with a process of conformational constraint of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of hepatitis C virusExpand
Severe acute respiratory syndrome coronavirus entry into host cells: Opportunities for therapeutic intervention†
The structure and function of the SARS CoV S protein is reviewed in the context of its role in virus entry and opportunities for the design and development of anti‐SARS agents based on the inhibition of receptor binding, the therapeutic uses of S‐directed monoclonal antibodies and inhibitors of HR1–HR2 complex formation are presented. Expand